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CAS No. :	484-12-8
Formula :	C₁₅H₁₆O₃
M.W :	244.29
SMILES Code :	C1=CC(=C(C2=C1C=CC(O2)=O)CC=C(C)C)OC
Synonyms :	Osthol; NSC 31868; Ostol
MDL No. :	MFCD00076049
InChI Key :	MBRLOUHOWLUMFF-UHFFFAOYSA-N
Pubchem ID :	10228

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

ATDC5 cells	0, 10, 50, 100 µM	1 week	Osthole promoted chondrogenesis in a dose-dependent manner, up-regulating the expression of chondrocyte-related marker genes (Sox9, Col2a1, and Col10a1)	Int J Biol Sci. 2017 Jul 18;13(8):996-1007.
HSC-T6 cells	1, 3, 10 μg/ml	24 hours	To evaluate the inhibitory effects of osthole on migration and invasion of HSC-T6 cells, results showed that osthole significantly inhibited TGF-β1-induced migration and invasion of HSC-T6 cells	J Biomed Sci. 2015 Aug 1;22(1):63.
LX-2 cells	1, 3, 10 μg/ml	24 hours	To evaluate the inhibitory effects of osthole on migration and invasion of LX-2 cells, results showed that osthole significantly inhibited TGF-β1-induced migration and invasion of LX-2 cells	J Biomed Sci. 2015 Aug 1;22(1):63.
Murine primary hepatocytes	40 µM	24 hours	Osthole did not alleviate APAP-induced cell death, but it significantly suppressed APAP-caused elevation of inflammatory cytokines	Acta Pharmacol Sin. 2018 Jan;39(1):74-84.
Raw264.7 cells	40 µM	24 hours	Osthole did not alleviate APAP-induced cell death, but it significantly suppressed APAP-caused elevation of inflammatory cytokines	Acta Pharmacol Sin. 2018 Jan;39(1):74-84.
Human Trabecular Meshwork (HTM) cells	10 µM	24 hours	Osthole significantly inhibited TGF-β2-induced expression of fibronectin (FN), collagen type IV (COL-IV), and laminin (LN), reversing the effects of TGF-β2.	Invest Ophthalmol Vis Sci. 2020 Aug 3;61(10):38.
MDA-MB-231	2, 5, 10, 25, 50 μg/mL	24 or 48 hours	Osthole significantly inhibited the proliferation of MDA-MB-231 cells with an IC50 value of 24.2 μg/mL (48 hours).	Acta Pharmacol Sin. 2022 Jun;43(6):1544-1555.
MDA-MB-231BO	2, 5, 10, 25, 50 μg/mL	24 or 48 hours	Osthole significantly inhibited the proliferation of MDA-MB-231BO cells with an IC50 value of 6.8 μg/mL (48 hours).	Acta Pharmacol Sin. 2022 Jun;43(6):1544-1555.
MCF-7	2, 5, 10, 25, 50 μg/mL	24 or 48 hours	Osthole significantly inhibited the proliferation of MCF-7 cells with an IC50 value of 123.9 μg/mL (48 hours).	Acta Pharmacol Sin. 2022 Jun;43(6):1544-1555.
MCF-10A	2, 5, 10, 25, 50 μg/mL	24 or 48 hours	Osthole showed low cytotoxicity to normal mammary epithelial cells MCF-10A with an IC50 value of 8944.0 μg/mL (48 hours).	Acta Pharmacol Sin. 2022 Jun;43(6):1544-1555.
MDA-MB-231	6.25, 12.5, 25, 50, 100, 200, 400, 800 µM	24, 48, 72 hours	Osthole inhibited the growth of MDA-MB-231 cells with an IC50 value of 129.4 μM at 24 hours.	J Exp Clin Cancer Res. 2018 Dec 22;37(1):322.
BT-549	6.25, 12.5, 25, 50, 100, 200, 400, 800 µM	24, 48, 72 hours	Osthole inhibited the growth of BT-549 cells with an IC50 value of 106.2 μM at 24 hours.	J Exp Clin Cancer Res. 2018 Dec 22;37(1):322.
MDA-MB-468	6.25, 12.5, 25, 50, 100, 200, 400, 800 µM	24, 48, 72 hours	Osthole inhibited the growth of MDA-MB-468 cells with an IC50 value of 105.4 μM at 24 hours.	J Exp Clin Cancer Res. 2018 Dec 22;37(1):322.
MCF-7	6.25, 12.5, 25, 50, 100, 200, 400, 800 µM	24, 48, 72 hours	Osthole inhibited the growth of MCF-7 cells with an IC50 value of 168 μM at 24 hours.	J Exp Clin Cancer Res. 2018 Dec 22;37(1):322.
LAD2 cells	72 and 144 µM	30 minutes	Osthole significantly reduced Ca2+ mobilization and degranulation in LAD2 cells in response to MRGPRX2 ligands (compound 48/80, substance P, and LL-37).	Front Immunol. 2020 Apr 24;11:703.
RBL-2H3 cells	72 µM	30 minutes	Osthole significantly reduced Ca2+ mobilization and degranulation in RBL-2H3 cells in response to MRGPRX2 ligands (compound 48/80, substance P, and LL-37).	Front Immunol. 2020 Apr 24;11:703.
Human skin mast cells	72 and 144 µM	30 minutes	Osthole significantly reduced degranulation in human skin mast cells in response to MRGPRX2 ligands (compound 48/80, substance P, and LL-37).	Front Immunol. 2020 Apr 24;11:703.
ATDC5 cells	0, 10, 50, 100 µM	one week	Osthole promoted chondrogenesis in a dose-dependent manner, significantly up-regulating the expression of chondrocyte-related marker genes (Sox9, Col2a1, and Col10a1).	Int J Biol Sci. 2017 Jul 18;13(8):996-1007.

Sprague-Dawley rats	Thioacetamide-induced hepatic fibrosis model	Oral gavage	10 mg/kg	Twice daily for 4 weeks	To evaluate the therapeutic effects of osthole on thioacetamide-induced hepatic fibrosis, results showed that osthole significantly reduced liver injury, improved hepatic fibrosis scores, and inhibited HSC activation	J Biomed Sci. 2015 Aug 1;22(1):63.
C57BL/6 mice	Paw edema model	Intraperitoneal injection	100 mg/kg	Once daily for 3 days	Osthole significantly reduced compound 48/80-induced paw edema and vascular leakage.	Front Immunol. 2020 Apr 24;11:703.
BALB/C mice	APAP-induced liver injury model	Intraperitoneal injection	100 mg/kg	Once daily for 3 days	Pretreatment with osthole significantly attenuated APAP-induced hepatocyte necrosis and the increases in ALT and AST activities. Compared with the mice treated with APAP alone, osthole pretreatment significantly reduced serum MDA levels and hepatic H2O2 levels, and improved liver GSH levels and the GSSG-to-GSH ratio. Meanwhile, osthole pretreatment markedly alleviated the APAP-induced up-regulation of inflammatory cytokines in the livers, and inhibited the expression of hepatic cytochrome P450 enzymes, but it increased the expression of hepatic UDP-glucuronosyltransferases (UGTs) and sulfotransferases (SULTs)	Acta Pharmacol Sin. 2018 Jan;39(1):74-84.
BALB/C mice	TMX-induced acute liver injury model	Intraperitoneal injection	100 mg/kg	Single injection, lasting 24 hours	Pretreatment with osthole significantly attenuated TMX-induced liver injury, evidenced by dose-dependent reduction of serum ALT and AST activities. Osthole also blunted TMX-induced oxidative stress, evidenced by significant increase of reduced glutathione (GSH) as well as reduction of malondialdehyde (MDA) and hydrogen peroxide (H2O2). Furthermore, osthole significantly enhanced the expressions of antioxidant genes (GPX1, SOD2, GCL-c, and G6pdh), but suppressed those of pro-oxidant genes (NOX2 and ACOX).	Acta Pharmacol Sin. 2019 May;40(5):608-619
BALB/c nu/nu female mice	MDA-MB-231 xenograft model	Intraperitoneal injection	100 or 200 mg/kg/d	Twice daily for 48 days	Osthole significantly reduced the volume and weight of MDA-MB-231 xenograft tumors and decreased the phosphorylation levels of STAT3.	J Exp Clin Cancer Res. 2018 Dec 22;37(1):322.
BALB/c mice	Ovalbumin-induced asthma model	Intraperitoneal injection	25 and 50 mg/kg	Once daily for 7 days	Osthole significantly reduced airway hyper-responsiveness and inflammatory cell infiltration in asthmatic mice, inhibited the release of Th2-type cytokines, and upregulated the IFN-γ level. Additionally, osthole significantly attenuated the expression of IL-33 and ST2 in the lungs of asthmatic mice.	Int J Mol Med. 2020 Oct;46(4):1389-1398
Zebrafish	Zebrafish breast cancer xenograft model	Embryo medium	3, 10, 20 μmol/L	48 hours	Osthole significantly reduced the dissemination of MDA-MB-231BO cells in zebrafish in a dose-dependent manner, decreasing the mean fluorescence intensity of tumor cells.	Acta Pharmacol Sin. 2022 Jun;43(6):1544-1555.
C57BL/6 mice	Tibial fracture model	Local subcutaneous injection	30 mg/kg	Once daily for 28 days	Osthole promotes bone fracture healing by activating BMP2 signaling, increasing cartilage and bone volume, and enhancing mechanical strength	Int J Biol Sci. 2017 Jul 18;13(8):996-1007.
C57BL/6 mice	Tibial fracture model	Local subcutaneous injection	30 mg/kg	Once daily for 28 days	Osthole promotes bone fracture healing by activating BMP2 signaling, significantly increasing bone volume and mechanical strength at the fracture site.	Int J Biol Sci. 2017 Jul 18;13(8):996-1007.
BALB/cJ mice	TGF-β2-induced ocular hypertension model	Intraperitoneal injection	30 mg/kg	Daily for 60 days	Osthole significantly reduced TGF-β2-induced ocular hypertension in mice and decreased the expression of FN, COL-IV, and LN in the trabecular meshwork tissue.	Invest Ophthalmol Vis Sci. 2020 Aug 3;61(10):38.
Wistar rats	Diet-induced metabolic syndrome model	Oral	40 mg/kg/d	Once daily for 30 days	To evaluate the preventive effect of Osthole on heart damage induced by metabolic syndrome. Results showed that Osthole reversed cardiac hypertrophy, local hypoxia, oxidative stress, and increased KHK activity and expression.	Antioxidants (Basel). 2023 Apr 28;12(5):1023

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CAS No.: 484-12-8

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CAS No.: 484-12-8

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Precautionary Statements-General

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Preparing Stock Solutions		1mg	5mg	10mg
Preparing Stock Solutions	1 mM 5 mM 10 mM	4.09mL 0.82mL 0.41mL	20.47mL 4.09mL 2.05mL	40.93mL 8.19mL 4.09mL
Dissolving Methods	Animal experiment 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

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