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Chemical Structure| 263707-16-0 Chemical Structure| 263707-16-0
Chemical Structure| 263707-16-0

ESI-09

CAS No.: 263707-16-0

ESI-09 is selective inhibitor of EPAC1 and EPAC2 with IC50 of 3.2 μM and 1.4 μM.

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Cat. No.: A248229 Purity: 98%

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Product Details of ESI-09

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

Safety of ESI-09

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of ESI-09

GPCR

Isoform Comparison

Biological Activity

Target
  • EPAC1

    EPAC1, IC50:3.2 μM

  • EPAC2

    EPAC2, IC50:1.4 μM

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

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.02mL

0.60mL

0.30mL

15.12mL

3.02mL

1.51mL

30.23mL

6.05mL

3.02mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

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