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CAS No.: 407587-33-1

CaCCinh-A01 Catalog No. CSN22911

Synonyms: TMEM16 Blocker I;CaCC(inh)-A01

CaCCinh-A01 is a dual inhibitor of TMEM16A and calcium-activated chloride channel (CaCC) with IC50s of 2.1 and 10 μM respectively.

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400-920-2911

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生物活性

实验方案

技术信息

生物活性

描述CaCCinh-A01 is an inhibitor of both TMEM16A and calcium-activated chloride channel (CaCC) with IC50s of 2.1 and 10 μM, respectively. 30 μM CaCCinh-A01 and 100 μM tannic acid strongly inhibit CaCC current following ATP stimulation^[1]. Adrenaline activates transient Cl(-) secretion and sustained K(+) secretion across isolated distal colonic mucosa of guinea-pigs. The Ca(2+)-activated Cl(-) channel inhibitor CaCCinh-A01 (30 μM) significantly reduced electrogenic K(+) secretion, detected as short-circuit current (I(sc)). CaCCinh-A01 inhibited both I(sc) and transepithelial conductance in a concentration-dependent manner (IC50 = 6.3 μM). In contrast to K(+) secretion, CaCCinh-A01 augmented the electrogenic Cl(-) secretion activated by adrenaline as well as that activated by prostaglandin E(2). Synergistic Cl(-) secretion activated by cholinergic/prostaglandin E(2) stimulation was insensitive to CaCCinh-A01^[2]. Intrathecal administration of selective CaCCs inhibitors (T16Ainh-A01 and CaCCinh-A01) also dose-dependently diminished tactile allodynia and thermal hyperalgesia. In addition, repeated administration of CaCCs inhibitors (T16Ainh-A01, CaCCinh-A01 or NFA) or anti-anoctamin-1 antibody prevented spinal nerve ligation-induced rises in anoctamin-1 mRNA and protein expression. Following spinal nerve ligation, the compound action potential generation of putative C fibers increased while selective CaCCs inhibitors (T16Ainh-A01 and CaCCinh-A01) attenuated such increase^[3].
参考文献

[1] Namkung W, Phuan PW, Verkman AS. TMEM16A inhibitors reveal TMEM16A as a minor component of calcium-activated chloride channel conductance in airway and intestinal epithelial cells. J Biol Chem. 2011;286(3):2365‐2374
[2] He Q, Halm ST, Zhang J, Halm DR. Activation of the basolateral membrane Cl- conductance essential for electrogenic K+ secretion suppresses electrogenic Cl- secretion. Exp Physiol. 2011;96(3):305‐316
[3] Pineda-Farias JB, Barragán-Iglesias P, Loeza-Alcocer E, et al. Role of anoctamin-1 and bestrophin-1 in spinal nerve ligation-induced neuropathic pain in rats. Mol Pain. 2015;11:41.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8783 mL
- 14.3914 mL
- 28.7829 mL
- 5 mM
- 0.5757 mL
- 2.8783 mL
- 5.7566 mL
- 10 mM
- 0.2878 mL
- 1.4391 mL
- 2.8783 mL

技术信息

CAS号

407587-33-1

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H21NO4S

运输

蓝冰

分子量

347.43

别名

TMEM16 Blocker I;CaCC(inh)-A01

溶解度

DMSO	300.0 mg/mL (863.5 mM)
Water	insoluble

动物实验配方

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