BCTC (CAS 393514-24-4)

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应用； BCTC is an effective and potent TRPV1 channel antagonist

CAS号码: 393514-24-4

纯度: ≥98%

分子量: 372.9

分子式: C₂₀H₂₅ClN₄O

仅供科研使用。不可用于诊断或治疗。

* 参考分析证明大量特定数据 (包括水含量).

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BTBC is an effective and potent transient receptor potential VR1 (vanilloid-1, TRPV1) channel antagonist. VR1 (TRPV1) is a Capsaicin (sc-3577) receptor that behaves as a non-selective cation channel that is mainly found in the sensory neurons, and specifically detects painful stimuli, low pH and heat. Studies show that BTBC and Capsazepine (sc-201098) both inhibit the activation of rat VR1 (vanilloid receptor 1), induced with acid or Capsaicin. Other VR1 (TRPV1) antagonists include AMG9810 (sc-201477) and SB705498. BCTC is an inhibitor of ANKTM1 and TRPM8.

参考文献

1. Valenzano, K.J., et al. 2003. J. Pharmacol. Exp. Therap. 306: 377-386. PMID: 12721338
2. Pomonis, J.D., et al. 2003. J. Pharmacol. Exp. Therap. 306: 387-393. PMID: 12721336
3. Tékus, V., et al. 2010. Eur. J. Pharmacol. 641: 135-141. PMID: 20534382
4. Schumacher, M.A. and Eilers, H. 2010. Front. Biosci. 15: 872-882. PMID: 20515731

物理状态 :

Solid

溶解度 :

Soluble in DMSO (20 mg/ml), ethanol (15 mg/ml with warming), and DMF.

保存 :

Store at room temperature

熔点 :

150-152° C

沸点 :

~561.58° C at 760 mmHg (Predicted)

密度 :

~1.23 g/cm³ (Predicted)

折射率 :

n²⁰_D 1.61 (Predicted)

IC50 :

capsaicin-induced TRPV1 receptors: IC₅₀ = 35 nM (rat); acid-induced TRPV1 receptors: IC₅₀ = 6 nM (rat); Vanilloid receptor: IC₅₀ = 0.7 nM (Rattus norvegicus); TRPA1 : EC₅₀50 = 4500 nM (human); Vanilloid receptor: IC₅₀ = 0.5 nM (human)

pK值 :

pK_a: 13.95, pK_b: 6.14

仅供科研使用。不可用于诊断或治疗。

PubChem CID :

9929425

SMILES :

CC(C)(C)C1=CC=C(C=C1)NC(=O)N2CCN(CC2)C3=C(C=CC=N3)Cl

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