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JNJ-17203212

Cat. No. M10840
JNJ-17203212  Structure
Size Price Availability Quantity
5mg USD 95  USD95 In stock
10mg USD 155  USD155 In stock
25mg USD 365  USD365 In stock
50mg USD 600  USD600 In stock
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Quality Control & Documentation
Biological Activity

JNJ-17203212 is a selective, highly effective, competitive TRPV1 antagonist. JNJ-17203212 was developed for research on pain management, such as migraines.

Chemical Information
Molecular Weight 419.32
Formula C17H15F6N5O
CAS Number 821768-06-3
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Fan Deng, et al. Gut Microbes. The gut microbiota metabolite capsiate promotes Gpx4 expression by activating TRPV1 to inhibit intestinal ischemia reperfusion-induced ferroptosis

[2] Xiuping Gao, et al. PLoS One. Cross-effect of TRPV1 and EP3 receptor on coughs and bronchopulmonary C-neural activities

[3] Jannis E Meents, et al. J Headache Pain. Two TRPV1 receptor antagonists are effective in two different experimental models of migraine

[4] S Kelly, et al. Ann Rheum Dis. Increased function of pronociceptive TRPV1 at the level of the joint in a rat model of osteoarthritis pain

[5] B J Wiskur, et al. Methods Find Exp Clin Pharmacol. A novel TRPV1 receptor antagonist JNJ-17203212 attenuates colonic hypersensitivity in rats

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