*Storage:
*Shipping:
ESI-09 is selective inhibitor of EPAC1 and EPAC2 with IC50 of 3.2 μM and 1.4 μM.
4.5
*For Research Use Only !
Change View
Size | Price | US Stock | Global Stock | In Stock |
1mg | łËò¶ÊÊ | Inquiry | Inquiry | |
5mg | ł§Ë¶ÊÊ | Inquiry | Inquiry | |
10mg | ł§î¶ÊÊ | Inquiry | Inquiry | |
25mg | łÍď¶ÊÊ | Inquiry | Inquiry | |
50mg | łòʶÊÊ | Inquiry | Inquiry | |
100mg | łďó¶ÊÊ | Inquiry | Inquiry | |
250mg | łÇÍî¶ÊÊ | Inquiry | Inquiry | |
1g | ł§îî¶ÊÊ | Inquiry | Inquiry |
US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks
łËò¶ÊÊ
ł§Ë¶ÊÊ
ł§î¶ÊÊ
łÍď¶ÊÊ
łòʶÊÊ
łďó¶ÊÊ
łÇÍî¶ÊÊ
ł§îî¶ÊÊ
In Stock
- +
US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
CAS No. : | 263707-16-0 |
Formula : | C16H15ClN4O2 |
M.W : | 330.77 |
SMILES Code : | O=C(C1=NOC(C(C)(C)C)=C1)/C(C#N)=N/NC2=CC(Cl)=CC=C2 |
MDL No. : | N/A |
InChI Key : | DXEATJQGQHDURZ-DEDYPNTBSA-N |
Pubchem ID : | 6077765 |
GHS Pictogram: | ![]() |
Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
Target |
|
In Vitro:
Cell Line
| Concentration | Treated Time | Description | Reference |
Rat urothelium-denuded detrusor strips | 10 μM | 15 minutes | ESI-09 prevented isoprenaline-induced adenosine release from rat detrusor strips, indicating the role of EPAC1 in β3-adrenoceptor-induced adenosine release. | PMC7060368 |
Human urothelium-denuded detrusor strips | 10 μM | 15 minutes | ESI-09 prevented mirabegron- and isoprenaline-induced adenosine release from human detrusor strips, indicating the role of EPAC1 in β3-adrenoceptor-induced adenosine release. | PMC7060368 |
Mouse airway smooth muscle cells (ASMCs) | 1, 10, 100 μM | 24, 48, 72 hours | ESI-09 promoted ASMCs proliferation at 10 and 100 μM | PMC6921488 |
Human umbilical vein endothelial cells (HUVECs) | 5 μM | 30 minutes | To evaluate the effect of ESI-09 on the attachment and invasion of Rickettsia australis into HUVECs. Results showed that ESI-09 significantly reduced intracellular and total bacterial counts. | PMC3845138 |
Mouse airway smooth muscle cells (ASMCs) | 1, 10, 100 μM | 30 minutes | ESI-09 promoted SOCE in ASMCs at 10 and 100 μM | PMC6921488 |
Left atrial fibroblasts | 1 μM | 48 hours | To evaluate the effect of Epac1 inhibition on isoproterenol's effect. ESI-09 blocked the isoproterenol-induced decrease in collagen protein expression. | PMC6302269 |
Left atrial fibroblasts | 1 μM | 48 hours | To evaluate the effect of Epac1 inhibition on collagen expression. ESI-09 increased COL1A1 mRNA levels by 40% and collagen I protein expression by 97%. | PMC6302269 |
A549 cells | 2 μM | 48 hours | Evaluate the effect of ESI-09 on lung cancer cell survival under low-glucose conditions, results showed ESI-09 significantly reduced cell survival | PMC7578269 |
Mouse airway smooth muscle cells (ASMCs) | 1, 10, 100 μM | 48 hours | ESI-09 had no significant effect on ASMCs apoptosis | PMC6921488 |
PC3 cells | 2 μM | 72 hours | Evaluate the effect of ESI-09 on lung cancer cell survival under low-glucose conditions, results showed ESI-09 significantly reduced cell survival | PMC7578269 |
H1975 cells | 2 μM | 72 hours | Evaluate the effect of ESI-09 on lung cancer cell survival under low-glucose conditions, results showed ESI-09 significantly reduced cell survival | PMC7578269 |
H1299 cells | 2 μM | 72 hours | Evaluate the effect of ESI-09 on lung cancer cell survival under low-glucose conditions, results showed ESI-09 significantly reduced cell survival | PMC7578269 |
MCF-7 breast cancer cells | 1 µM | 72 hours | ESI-09, as an EPAC inhibitor, abrogated the isoprenaline-induced lipid droplet accumulation | PMC9820888 |
Human atrial myocytes | 10 μM | ESI-09, as an Epac inhibitor, reversed or prevented the noradrenaline-induced up-regulation of ICl.vol under hypotonic conditions | PMC6057899 |
In Vivo:
Species
| Animal Model
| Administration | Dosage | Frequency | Description | Reference |
Rats | Neonatal colorectal distension (CRD)-induced visceral hypersensitivity model | Intra-PVN microinjection | 1.0 μg/μl | Single injection, needle retained for 10 minutes | Inhibition of Epac1 increased the firing frequency of PVN CRF neurons, facilitated visceral hypersensitivity and pain precipitation | PMC9344090 |
Mice | Orthotopic metastatic PDA mouse model | Intraperitoneal injection | 10 mg/kg | 3 weeks | Reduced local and distant spread of MIA PaCa-2 cells and significantly decreased metastasis to the liver | PMC4769034 |
Female BALB/c mice | Acute and chronic asthma models | Intraperitoneal injection | 10 mg/kg | 30 min before each OVA challenge for 3 days (acute) or 6 weeks (chronic) | ESI-09 aggravated airway inflammation and airway remodeling | PMC6921488 |
Mice (C57BL/6) | Fatal spotted fever group (SFG) rickettsiosis model | Intraperitoneal injection | 10 mg/kg/day | Once daily for 5 days before infection and 7 days after infection | To evaluate the therapeutic effect of ESI-09 on fatal SFG rickettsiosis. Results showed that ESI-09 significantly improved survival and reduced pathological damage. | PMC3845138 |
Mice | Epac WT, Epac1–/–, Epac2–/–, and Epac1&2–/– mice | Intraperitoneal injection | 10 mg/kgBW | Daily injections for 7 days | To investigate the effect of ESI-09 on urinary sodium excretion in mice, results showed that ESI-09 significantly increased urinary sodium excretion under a low-sodium diet, indicating its inhibitory effect on ENaC activity. | PMC8855822 |
Rat | Urethane-anaesthetized rats | Intravesical instillation | 10 μM | Single administration | Pre-treatment with ESI-09 prevented the reduction of the voiding frequency caused by isoprenaline and forskolin, indicating the role of EPAC1 in β3-adrenoceptor-induced bladder function regulation. | PMC7060368 |
BALB/c-nu (nu/nu) mice | A549 cell xenograft model | Intraperitoneal injection | 2 mg/kg or 10 mg/kg | Once daily for 21 days | Evaluate the inhibitory effect of ESI-09 on tumor growth, results showed ESI-09 significantly inhibited tumor growth and reduced tumor volume | PMC7578269 |
C57Bl/6 mice | GDNF-induced hyperalgesic priming model | Oral | 20 mg/kg | Administered on the 13th and 14th day | ESI-09 significantly reduced the duration of PGE2 hyperalgesia in GDNF-primed mice. | PMC5996251 |
C57BL/6 mice | Myocardial infarction model | Intraperitoneal injection | 20 mg/kg/day | Once daily for 5 days | To evaluate the effect of Epac1 inhibition post-MI. ESI-09 did not significantly alter the heart weight to body weight ratio, LV function, or atrial fibrosis. | PMC6302269 |
Rats | Chronic morphine-induced analgesic tolerance model | Intrathecal injection | 5 μg | Once daily for 7 days | ESI-09 significantly attenuated the development of morphine-induced anti-nociceptive tolerance while retaining the anti-nociceptive effect of morphine. Additionally, ESI-09 reduced the phosphorylation of PKC ε and up-regulated expression of Epac after chronic morphine exposure. | PMC5913404 |
Mice | CFA-induced inflammatory mechanical hyperalgesia model | Oral | 5, 20, or 50 mg/kg | Treatment started on the third day after CFA administration | To evaluate the inhibitory effect of ESI-09 on established CFA-induced mechanical hyperalgesia | PMC4801297 |
Tags: ESI-09 | ESI09 | ESI 09 | Virus Protease | Exchange Protein directly Activated by cAMP | EPAC antagonist | EPAC1 antagonist | EPAC2 antagonist | cAMP-dependent signaling | immune response | cell migration | virus replication | Virus Protease Inhibitor | 263707-16-0
Precautionary Statements-General | |
Code | Phrase |
P101 | If medical advice is needed,have product container or label at hand. |
P102 | Keep out of reach of children. |
P103 | Read label before use |
Prevention | |
Code | Phrase |
P201 | Obtain special instructions before use. |
P202 | Do not handle until all safety precautions have been read and understood. |
P210 | Keep away from heat/sparks/open flames/hot surfaces. - No smoking. |
P211 | Do not spray on an open flame or other ignition source. |
P220 | Keep/Store away from clothing/combustible materials. |
P221 | Take any precaution to avoid mixing with combustibles |
P222 | Do not allow contact with air. |
P223 | Keep away from any possible contact with water, because of violent reaction and possible flash fire. |
P230 | Keep wetted |
P231 | Handle under inert gas. |
P232 | Protect from moisture. |
P233 | Keep container tightly closed. |
P234 | Keep only in original container. |
P235 | Keep cool |
P240 | Ground/bond container and receiving equipment. |
P241 | Use explosion-proof electrical/ventilating/lighting/equipment. |
P242 | Use only non-sparking tools. |
P243 | Take precautionary measures against static discharge. |
P244 | Keep reduction valves free from grease and oil. |
P250 | Do not subject to grinding/shock/friction. |
P251 | Pressurized container: Do not pierce or burn, even after use. |
P260 | Do not breathe dust/fume/gas/mist/vapours/spray. |
P261 | Avoid breathing dust/fume/gas/mist/vapours/spray. |
P262 | Do not get in eyes, on skin, or on clothing. |
P263 | Avoid contact during pregnancy/while nursing. |
P264 | Wash hands thoroughly after handling. |
P265 | Wash skin thouroughly after handling. |
P270 | Do not eat, drink or smoke when using this product. |
P271 | Use only outdoors or in a well-ventilated area. |
P272 | Contaminated work clothing should not be allowed out of the workplace. |
P273 | Avoid release to the environment. |
P280 | Wear protective gloves/protective clothing/eye protection/face protection. |
P281 | Use personal protective equipment as required. |
P282 | Wear cold insulating gloves/face shield/eye protection. |
P283 | Wear fire/flame resistant/retardant clothing. |
P284 | Wear respiratory protection. |
P285 | In case of inadequate ventilation wear respiratory protection. |
P231 + P232 | Handle under inert gas. Protect from moisture. |
P235 + P410 | Keep cool. Protect from sunlight. |
Response | |
Code | Phrase |
P301 | IF SWALLOWED: |
P304 | IF INHALED: |
P305 | IF IN EYES: |
P306 | IF ON CLOTHING: |
P307 | IF exposed: |
P308 | IF exposed or concerned: |
P309 | IF exposed or if you feel unwell: |
P310 | Immediately call a POISON CENTER or doctor/physician. |
P311 | Call a POISON CENTER or doctor/physician. |
P312 | Call a POISON CENTER or doctor/physician if you feel unwell. |
P313 | Get medical advice/attention. |
P314 | Get medical advice/attention if you feel unwell. |
P315 | Get immediate medical advice/attention. |
P320 | |
P302 + P352 | IF ON SKIN: wash with plenty of soap and water. |
P321 | |
P322 | |
P330 | Rinse mouth. |
P331 | Do NOT induce vomiting. |
P332 | IF SKIN irritation occurs: |
P333 | If skin irritation or rash occurs: |
P334 | Immerse in cool water/wrap n wet bandages. |
P335 | Brush off loose particles from skin. |
P336 | Thaw frosted parts with lukewarm water. Do not rub affected area. |
P337 | If eye irritation persists: |
P338 | Remove contact lenses, if present and easy to do. Continue rinsing. |
P340 | Remove victim to fresh air and keep at rest in a position comfortable for breathing. |
P341 | If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing. |
P342 | If experiencing respiratory symptoms: |
P350 | Gently wash with plenty of soap and water. |
P351 | Rinse cautiously with water for several minutes. |
P352 | Wash with plenty of soap and water. |
P353 | Rinse skin with water/shower. |
P360 | Rinse immediately contaminated clothing and skin with plenty of water before removing clothes. |
P361 | Remove/Take off immediately all contaminated clothing. |
P362 | Take off contaminated clothing and wash before reuse. |
P363 | Wash contaminated clothing before reuse. |
P370 | In case of fire: |
P371 | In case of major fire and large quantities: |
P372 | Explosion risk in case of fire. |
P373 | DO NOT fight fire when fire reaches explosives. |
P374 | Fight fire with normal precautions from a reasonable distance. |
P376 | Stop leak if safe to do so. Oxidising gases (section 2.4) 1 |
P377 | Leaking gas fire: Do not extinguish, unless leak can be stopped safely. |
P378 | |
P380 | Evacuate area. |
P381 | Eliminate all ignition sources if safe to do so. |
P390 | Absorb spillage to prevent material damage. |
P391 | Collect spillage. Hazardous to the aquatic environment |
P301 + P310 | IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician. |
P301 + P312 | IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. |
P301 + P330 + P331 | IF SWALLOWED: Rinse mouth. Do NOT induce vomiting. |
P302 + P334 | IF ON SKIN: Immerse in cool water/wrap in wet bandages. |
P302 + P350 | IF ON SKIN: Gently wash with plenty of soap and water. |
P303 + P361 + P353 | IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower. |
P304 + P312 | IF INHALED: Call a POISON CENTER or doctor/physician if you feel unwell. |
P304 + P340 | IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing. |
P304 + P341 | IF INHALED: If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing. |
P305 + P351 + P338 | IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. |
P306 + P360 | IF ON CLOTHING: Rinse Immediately contaminated CLOTHING and SKIN with plenty of water before removing clothes. |
P307 + P311 | IF exposed: call a POISON CENTER or doctor/physician. |
P308 + P313 | IF exposed or concerned: Get medical advice/attention. |
P309 + P311 | IF exposed or if you feel unwell: call a POISON CENTER or doctor/physician. |
P332 + P313 | IF SKIN irritation occurs: Get medical advice/attention. |
P333 + P313 | IF SKIN irritation or rash occurs: Get medical advice/attention. |
P335 + P334 | Brush off loose particles from skin. Immerse in cool water/wrap in wet bandages. |
P337 + P313 | IF eye irritation persists: Get medical advice/attention. |
P342 + P311 | IF experiencing respiratory symptoms: call a POISON CENTER or doctor/physician. |
P370 + P376 | In case of fire: Stop leak if safe to Do so. |
P370 + P378 | In case of fire: |
P370 + P380 | In case of fire: Evacuate area. |
P370 + P380 + P375 | In case of fire: Evacuate area. Fight fire remotely due to the risk of explosion. |
P371 + P380 + P375 | In case of major fire and large quantities: Evacuate area. Fight fire remotely due to the risk of explosion. |
Storage | |
Code | Phrase |
P401 | |
P402 | Store in a dry place. |
P403 | Store in a well-ventilated place. |
P404 | Store in a closed container. |
P405 | Store locked up. |
P406 | Store in corrosive resistant/ container with a resistant inner liner. |
P407 | Maintain air gap between stacks/pallets. |
P410 | Protect from sunlight. |
P411 | |
P412 | Do not expose to temperatures exceeding 50 oC/ 122 oF. |
P413 | |
P420 | Store away from other materials. |
P422 | |
P402 + P404 | Store in a dry place. Store in a closed container. |
P403 + P233 | Store in a well-ventilated place. Keep container tightly closed. |
P403 + P235 | Store in a well-ventilated place. Keep cool. |
P410 + P403 | Protect from sunlight. Store in a well-ventilated place. |
P410 + P412 | Protect from sunlight. Do not expose to temperatures exceeding 50 oC/122oF. |
P411 + P235 | Keep cool. |
Disposal | |
Code | Phrase |
P501 | Dispose of contents/container to ... |
P502 | Refer to manufacturer/supplier for information on recovery/recycling |
Physical hazards | |
Code | Phrase |
H200 | Unstable explosive |
H201 | Explosive; mass explosion hazard |
H202 | Explosive; severe projection hazard |
H203 | Explosive; fire, blast or projection hazard |
H204 | Fire or projection hazard |
H205 | May mass explode in fire |
H220 | Extremely flammable gas |
H221 | Flammable gas |
H222 | Extremely flammable aerosol |
H223 | Flammable aerosol |
H224 | Extremely flammable liquid and vapour |
H225 | Highly flammable liquid and vapour |
H226 | Flammable liquid and vapour |
H227 | Combustible liquid |
H228 | Flammable solid |
H229 | Pressurized container: may burst if heated |
H230 | May react explosively even in the absence of air |
H231 | May react explosively even in the absence of air at elevated pressure and/or temperature |
H240 | Heating may cause an explosion |
H241 | Heating may cause a fire or explosion |
H242 | Heating may cause a fire |
H250 | Catches fire spontaneously if exposed to air |
H251 | Self-heating; may catch fire |
H252 | Self-heating in large quantities; may catch fire |
H260 | In contact with water releases flammable gases which may ignite spontaneously |
H261 | In contact with water releases flammable gas |
H270 | May cause or intensify fire; oxidizer |
H271 | May cause fire or explosion; strong oxidizer |
H272 | May intensify fire; oxidizer |
H280 | Contains gas under pressure; may explode if heated |
H281 | Contains refrigerated gas; may cause cryogenic burns or injury |
H290 | May be corrosive to metals |
Health hazards | |
Code | Phrase |
H300 | Fatal if swallowed |
H301 | Toxic if swallowed |
H302 | Harmful if swallowed |
H303 | May be harmful if swallowed |
H304 | May be fatal if swallowed and enters airways |
H305 | May be harmful if swallowed and enters airways |
H310 | Fatal in contact with skin |
H311 | Toxic in contact with skin |
H312 | Harmful in contact with skin |
H313 | May be harmful in contact with skin |
H314 | Causes severe skin burns and eye damage |
H315 | Causes skin irritation |
H316 | Causes mild skin irritation |
H317 | May cause an allergic skin reaction |
H318 | Causes serious eye damage |
H319 | Causes serious eye irritation |
H320 | Causes eye irritation |
H330 | Fatal if inhaled |
H331 | Toxic if inhaled |
H332 | Harmful if inhaled |
H333 | May be harmful if inhaled |
H334 | May cause allergy or asthma symptoms or breathing difficulties if inhaled |
H335 | May cause respiratory irritation |
H336 | May cause drowsiness or dizziness |
H340 | May cause genetic defects |
H341 | Suspected of causing genetic defects |
H350 | May cause cancer |
H351 | Suspected of causing cancer |
H360 | May damage fertility or the unborn child |
H361 | Suspected of damaging fertility or the unborn child |
H361d | Suspected of damaging the unborn child |
H362 | May cause harm to breast-fed children |
H370 | Causes damage to organs |
H371 | May cause damage to organs |
H372 | Causes damage to organs through prolonged or repeated exposure |
H373 | May cause damage to organs through prolonged or repeated exposure |
Environmental hazards | |
Code | Phrase |
H400 | Very toxic to aquatic life |
H401 | Toxic to aquatic life |
H402 | Harmful to aquatic life |
H410 | Very toxic to aquatic life with long-lasting effects |
H411 | Toxic to aquatic life with long-lasting effects |
H412 | Harmful to aquatic life with long-lasting effects |
H413 | May cause long-lasting harmful effects to aquatic life |
H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
Sorry,this product has been discontinued.
Home
* Country/Region
* Quantity Required :
* Cat. No.:
* CAS No :
* Product Name :
* Additional Information :
Total Compounds: mg
The concentration of the dissolution solution you need to prepare is mg/mL