产品
编 号：F240475
分子式：C22H23ClFN3O2S
分子量：447.95
分子式：C22H23ClFN3O2S
分子量：447.95
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 1933528-96-1
产品详情
生物活性：
MDR-652 is a highly specific and efficacious transient receptor potential vanilloid 1 (TRPV1) ligand with agonist activity. The Kis are 11.4 and 23.8 nM for hTRPV1 and rTRPV1, respectively. The EC50s are 5.05 and 93 nM for hTRPV1 and rTRPV1, respectively. Potent topical analgesic activity.
体内研究：
MDR-652 (0.5 and 5 mg/kg) displays a dose-dependent decrease of body temperature, supporting that MDR-652 displays TRPV1 agonism in the intact animal.MDR-652 (5-10 mg/kg; i.p. ands.c.) blocks the neuropathic pain completely, indicating 100% maximum possible effect (MPE) . MDR-652 has a promising topical pharmacokinetic profile. MDR-652 has no significant toxicity. In a single-dose toxicity study, the LD50 of MDR-652 is higher than 200 and 2000 mg/kg in i.p. and p.o. administration, respectively.Animal Model:ICR mouse
Dosage:0.5 and 5 mg/kg
Administration:Administered intraperitoneally; 7 hours
Result:Decreased body temperature in a dose-dependent manner.
Animal Model:Rats with spinal nerve ligation (SNL) model
Dosage:1, 2, 5, and 10 mg/kg
Administration:Administered intraperitoneally and subcutaneously; 24 hours
Result:The i.p. administration exhibited an excellent and dose dependent analgesic profile with an ED50 of 0.5-2 mg/kg.The subcutaneous injection (sc) also displayed an excellent analgesic outcome with maximum effect at 30 min after administration.
MDR-652 is a highly specific and efficacious transient receptor potential vanilloid 1 (TRPV1) ligand with agonist activity. The Kis are 11.4 and 23.8 nM for hTRPV1 and rTRPV1, respectively. The EC50s are 5.05 and 93 nM for hTRPV1 and rTRPV1, respectively. Potent topical analgesic activity.
体内研究：
MDR-652 (0.5 and 5 mg/kg) displays a dose-dependent decrease of body temperature, supporting that MDR-652 displays TRPV1 agonism in the intact animal.MDR-652 (5-10 mg/kg; i.p. ands.c.) blocks the neuropathic pain completely, indicating 100% maximum possible effect (MPE) . MDR-652 has a promising topical pharmacokinetic profile. MDR-652 has no significant toxicity. In a single-dose toxicity study, the LD50 of MDR-652 is higher than 200 and 2000 mg/kg in i.p. and p.o. administration, respectively.Animal Model:ICR mouse
Dosage:0.5 and 5 mg/kg
Administration:Administered intraperitoneally; 7 hours
Result:Decreased body temperature in a dose-dependent manner.
Animal Model:Rats with spinal nerve ligation (SNL) model
Dosage:1, 2, 5, and 10 mg/kg
Administration:Administered intraperitoneally and subcutaneously; 24 hours
Result:The i.p. administration exhibited an excellent and dose dependent analgesic profile with an ED50 of 0.5-2 mg/kg.The subcutaneous injection (sc) also displayed an excellent analgesic outcome with maximum effect at 30 min after administration.
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