BCTC CAS: 393514-24-4
MF: C20H25ClN4O
MW: 372.9
An effective and potent TRPV1 channel antagonist.

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).

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 :
n20D 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 :
pKa: 13.95, pKb: 6.14
仅供科研使用。不可用于诊断或治疗。
PubChem CID :
SMILES :
CC(C)(C)C1=CC=C(C=C1)NC(=O)N2CCN(CC2)C3=C(C=CC=N3)Cl

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引用1 - 66

PMID: # 28865353  Souza, RF.|Oliveira, LL.|Nones, CFM.|Dos Reis, RC.|Araya, EI.|Kopruszinski, CM.|Rae, GA.|Chichorro, JG.| et al. 2017. Arch Oral Biol. 83: 297-303.

PMID: # 27392124  Dos Reis, RC.|Kopruszinski, CM.|Nones, CF.|Chichorro, JG.| et al. 2016. Behav Pharmacol. 27: 528-35.

PMID: # 12721338  Valenzano, KJ. et al. 2003. J. Pharmacol. Exp. Ther. 306: 377-386.

PMID: # 12721336  Pomonis, JD. et al. 2003. J. Pharmacol. Exp. Ther. 306: 387-393.

PMID: # 32758574  Eur. J. Pharmacol. 173357.

PMID: # 31654626  Biochem. Pharmacol. 113678.

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