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SB 366791

Catalog No.GC14997

SB 366791 es un potente y selectivo antagonista del receptor vaniloide (VR1/TRPV1) (IC50\u003d5,7 nM).

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SB 366791 Chemical Structure

Cas No.: 472981-92-3

Tamaño Precio Disponibilidad Cantidad
10mg
65,00 $
Disponible
50mg
222,00 $
Disponible

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Sample solution is provided at 25 µL, 10mM.

Description of SB 366791

SB-366791 is a potent , competitive and selective vanilloid receptor (VR1/TRPV1) antagonist with IC50 of 5.7±1.2 nMtarget: VR1/TRPV1IC 50: 5.7±1.2 nM [1] SB-366791 produced a concentration-dependent inhibition of the response to capsaicin with an apparent pKb of 7.74±0.08. Schild analysis indicated a competitive mechanism of action with a pA2 of 7.71.[1] SB-366791 showed a concentration-dependent potentiation of pH 5-induced 45Ca2+uptake in CHO cells expressing rat TRPV1 but not in untransfected cells[2]

References:
[1]. M.J. Gunthorpe et al. Identification and characterisation of SB-366791, a potent and selective vanilloid receptor (VR1/TRPV1) antagonist. Neuropharmacology, 2004 Jan, 46(1):133-49.
[2]. Gavva NR et al. Proton Activation Does Not Alter Antagonist Interaction with the Capsaicin-Binding Pocket of TRPV1. Mol Pharmacol, 2005 Dec, 68(6), 1524-33.

Chemical Properties of SB 366791

Cas No. 472981-92-3 SDF
Chemical Name (E)-3-(4-chlorophenyl)-N-(3-methoxyphenyl)acrylamide
Canonical SMILES ClC1=CC=C(C=C1)/C=C/C(NC2=CC=CC(OC)=C2)=O
Formula C16H14ClNO2 M.Wt 287.75
Solubility ≥ 12.35mg/mL in DMSO Storage Store at RT
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of SB 366791

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1 mg 5 mg 10 mg
1 mM 3.4752 mL 17.3762 mL 34.7524 mL
5 mM 0.695 mL 3.4752 mL 6.9505 mL
10 mM 0.3475 mL 1.7376 mL 3.4752 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 24 reference(s) in Google Scholar.)

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