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Mavatrep

Catalog No. T16014   CAS 956274-94-5
Synonyms: JNJ-39439335

Mavatrep (JNJ-39439335) is a selective antagonist of TRPV1 with Ki of 6.5 nM and can be used for studies about inflammatory pain.

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Mavatrep Chemical Structure
Mavatrep, CAS 956274-94-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 60.00
5 mg In stock $ 147.00
10 mg In stock $ 239.00
25 mg In stock $ 478.00
50 mg In stock $ 772.00
100 mg In stock $ 1,230.00
500 mg In stock $ 2,490.00
1 mL * 10 mM (in DMSO) In stock $ 162.00
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Purity: 98.01%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Mavatrep (JNJ-39439335) is a selective antagonist of TRPV1 with Ki of 6.5 nM and can be used for studies about inflammatory pain.
In vitro In cells expressing recombinant human TRPV1 channels, Mavatrep antagonized capsaicin-induced Ca2+ influx with an IC50 of 4.6 nM. Mavatrep blocked the activation of hTRPV1 channels by Capsaicin (1 μM, pH 5.0) in a concentration-dependent fashion[1].
In vivo In the complete Freund's adjuvant- and carrageenan-induced thermal hypersensitivity models, Mavatrep exhibited full efficacy, with ED80 values of 7.8 and 0.5 mg/kg, respectively, corresponding to plasma levels of 270.8 and 9.2 ng/mL, respectively. On the basis of Mavatrep superior pharmacologic and safety profile, Mavatrep was selected for clinical development for the treatment of pain[1].
Synonyms JNJ-39439335
Molecular Weight 422.44
Formula C25H21F3N2O
CAS No. 956274-94-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 16 mg/mL (37.88 mM), Sonication and heating to 60℃ are recommended.

TargetMolReferences and Literature

1. Parsons WH, et al. Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep). J Med Chem. 2015 May

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Inhibitor Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Membrane Protein-targeted Compound Library Neuronal Signaling Compound Library Anti-Cancer Compound Library Clinical Compound Library ReFRAME Related Library Human Metabolite Library

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Keywords

Mavatrep 956274-94-5 Membrane transporter/Ion channel TRP/TRPV Channel Inhibitor capsaicin TRP Channel neuropathic pain calcium ions JNJ-39439335 JNJ 39439335 inhibit Transient receptor potential channels hTRPV1 channel JNJ39439335 HEK293 inhibitor

 

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