CaCCinh-A01
CaCCinh-A01, also known as TMEM16 Blocker I, is a TMEM16 Blocker. CaCCinh-A01 is a non-selective inhibitor of calcium-activated chloride channels (CaCCs) that blocks ATP-stimulated chloride conductance in human salivary gland, intestinal, and bronchial epithelium (mean IC50 = 10 µM).
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | CaCCinh-A01 |
|---|---|
| Iupac 化学名称 | 6-(1,1-dimethylethyl)-2-[(2-furanylcarbonyl)amino]-4,5,6,7-tetrahydro-benzo[b]thiophene-3-carboxylic acid |
| 同义词 | CaCCinh-A01; CaCC(inh)-A01, TMEM16 Blocker I. |
| 英文同义词 | CaCCinh-A01; CaCC(inh)-A01, TMEM16 Blocker I. |
| 分子式 | C18H21NO4S |
| 分子量 | 347.429 |
| Smile | O=C(C1=C(NC(C2=CC=CO2)=O)SC3=C1CCC(C(C)(C)C)C3)O |
| InChiKey | ACLUEOBQFRYTQS-UHFFFAOYSA-N |
| InChi | InChI=1S/C18H21NO4S/c1-18(2,3)10-6-7-11-13(9-10)24-16(14(11)17(21)22)19-15(20)12-5-4-8-23-12/h4-5,8,10H,6-7,9H2,1-3H3,(H,19,20)(H,21,22) |
| Cas号 | 407587-33-1 |
| 相关CAS号 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 固体粉末 |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 干燥、黑暗，短期（日至周）0-4摄氏度，长期（月至年）0-20摄氏度。 |
| 可溶性 | 可溶于DMSO |
| 处理方式 | |
| 运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周。 |
| 海关编码 |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Hannigan KI, Griffin CS, Large RJ, Sergeant GP, Hollywood MA, McHale NG, Thornbury KD. The role of Ca(2+)-activated Cl(-) current in tone generation in the rabbit corpus cavernosum. Am J Physiol Cell Physiol. 2017 Nov 1;313(5):C475-C486. doi: 10.1152/ajpcell.00025.2017. Epub 2017 Aug 23. PubMed PMID: 28835432.
2: Fedigan S, Bradley E, Webb T, Large RJ, Hollywood MA, Thornbury KD, McHale NG, Sergeant GP. Effects of new-generation TMEM16A inhibitors on calcium-activated chloride currents in rabbit urethral interstitial cells of Cajal. Pflugers Arch. 2017 Jul 21. doi: 10.1007/s00424-017-2028-5. [Epub ahead of print] PubMed PMID: 28733893.
3: Banerjee J, Leung CT, Li A, Peterson-Yantorno K, Ouyang H, Stamer WD, Civan MM. Regulatory Roles of Anoctamin-6 in Human Trabecular Meshwork Cells. Invest Ophthalmol Vis Sci. 2017 Jan 1;58(1):492-501. doi: 10.1167/iovs.16-20188. PubMed PMID: 28125837; PubMed Central PMCID: PMC5283088.
4: Yu B, Jiang Y, Jin L, Ma T, Yang H. Role of Quercetin in Modulating Chloride Transport in the Intestine. Front Physiol. 2016 Nov 23;7:549. eCollection 2016. PubMed PMID: 27932986; PubMed Central PMCID: PMC5120089.
5: Guan L, Song Y, Gao J, Gao J, Wang K. Inhibition of calcium-activated chloride channel ANO1 suppresses proliferation and induces apoptosis of epithelium originated cancer cells. Oncotarget. 2016 Nov 29;7(48):78619-78630. doi: 10.18632/oncotarget.12524. PubMed PMID: 27732935; PubMed Central PMCID: PMC5346664.
6: Kamikawa A, Ichii O, Sakazaki J, Ishikawa T. Ca2+-activated Cl- channel currents in mammary secretory cells from lactating mouse. Am J Physiol Cell Physiol. 2016 Nov 1;311(5):C808-C819. doi: 10.1152/ajpcell.00050.2016. Epub 2016 Aug 24. PubMed PMID: 27558156.
7: Gianotti A, Ferrera L, Philp AR, Caci E, Zegarra-Moran O, Galietta LJ, Flores CA. Pharmacological analysis of epithelial chloride secretion mechanisms in adult murine airways. Eur J Pharmacol. 2016 Jun 15;781:100-8. doi: 10.1016/j.ejphar.2016.04.007. Epub 2016 Apr 7. PubMed PMID: 27063443.
8: Hwang SJ, Basma N, Sanders KM, Ward SM. Effects of new-generation inhibitors of the calcium-activated chloride channel anoctamin 1 on slow waves in the gastrointestinal tract. Br J Pharmacol. 2016 Apr;173(8):1339-49. doi: 10.1111/bph.13431. Epub 2016 Mar 6. PubMed PMID: 26774021; PubMed Central PMCID: PMC4940814.
9: Chatterjee T, Sheikh IA, Chakravarty D, Chakrabarti P, Sarkar P, Saha T, Chakrabarti MK, Hoque KM. Effects of Small Molecule Calcium-Activated Chloride Channel Inhibitors on Structure and Function of Accessory Cholera Enterotoxin (Ace) of Vibrio cholerae. PLoS One. 2015 Nov 5;10(11):e0141283. doi: 10.1371/journal.pone.0141283. eCollection 2015. PubMed PMID: 26540279; PubMed Central PMCID: PMC4634967.
10: Cherkashin AP, Kolesnikova AS, Tarasov MV, Romanov RA, Rogachevskaja OA, Bystrova MF, Kolesnikov SS. Expression of calcium-activated chloride channels Ano1 and Ano2 in mouse taste cells. Pflugers Arch. 2016 Feb;468(2):305-19. doi: 10.1007/s00424-015-1751-z. Epub 2015 Nov 3. PubMed PMID: 26530828.
11: Pineda-Farias JB, Barragán-Iglesias P, Loeza-Alcocer E, Torres-López JE, Rocha-González HI, Pérez-Severiano F, Delgado-Lezama R, Granados-Soto V. Role of anoctamin-1 and bestrophin-1 in spinal nerve ligation-induced neuropathic pain in rats. Mol Pain. 2015 Jul 1;11:41. doi: 10.1186/s12990-015-0042-1. PubMed PMID: 26130088; PubMed Central PMCID: PMC4487556.
12: Boedtkjer DM, Kim S, Jensen AB, Matchkov VM, Andersson KE. New selective inhibitors of calcium-activated chloride channels - T16A(inh) -A01, CaCC(inh) -A01 and MONNA - what do they inhibit? Br J Pharmacol. 2015 Aug;172(16):4158-72. doi: 10.1111/bph.13201. Epub 2015 Jul 8. PubMed PMID: 26013995; PubMed Central PMCID: PMC4543620.
13: Sanders KM, O'Driscoll K, Leblanc N. Pharmacological properties of native CaCCs and TMEM16A. Channels (Austin). 2014;8(6):473-4. doi: 10.4161/19336950.2014.986624. PubMed PMID: 25528999; PubMed Central PMCID: PMC4594607.
14: Sauter DRP, Novak I, Pedersen SF, Larsen EH, Hoffmann EK. ANO1 (TMEM16A) in pancreatic ductal adenocarcinoma (PDAC). Pflugers Arch. 2015 Jul;467(7):1495-1508. doi: 10.1007/s00424-014-1598-8. Epub 2014 Aug 28. PubMed PMID: 25163766; PubMed Central PMCID: PMC4464647.
15: Liu Y, Zhang H, Huang D, Qi J, Xu J, Gao H, Du X, Gamper N, Zhang H. Characterization of the effects of Cl⁻ channel modulators on TMEM16A and bestrophin-1 Ca²⁺ activated Cl⁻ channels. Pflugers Arch. 2015 Jul;467(7):1417-1430. doi: 10.1007/s00424-014-1572-5. Epub 2014 Aug 1. PubMed PMID: 25078708.
16: García G, Martínez-Rojas VA, Rocha-González HI, Granados-Soto V, Murbartián J. Evidence for the participation of Ca(2+)-activated chloride channels in formalin-induced acute and chronic nociception. Brain Res. 2014 Sep 4;1579:35-44. doi: 10.1016/j.brainres.2014.07.011. Epub 2014 Jul 15. PubMed PMID: 25036442.
17: Bill A, Hall ML, Borawski J, Hodgson C, Jenkins J, Piechon P, Popa O, Rothwell C, Tranter P, Tria S, Wagner T, Whitehead L, Gaither LA. Small molecule-facilitated degradation of ANO1 protein: a new targeting approach for anticancer therapeutics. J Biol Chem. 2014 Apr 18;289(16):11029-41. doi: 10.1074/jbc.M114.549188. Epub 2014 Mar 5. PubMed PMID: 24599954; PubMed Central PMCID: PMC4036244.
18: Qi J, Wang Y, Liu Y, Zhang F, Guan B, Zhang H. Development and validation of HTS assay for screening the calcium-activated chloride channel modulators in TMEM16A stably expressed CHO cells. Anal Bioanal Chem. 2014 Feb;406(6):1713-21. doi: 10.1007/s00216-013-7550-5. Epub 2014 Jan 22. PubMed PMID: 24448969.
19: Ko EA, Jin BJ, Namkung W, Ma T, Thiagarajah JR, Verkman AS. Chloride channel inhibition by a red wine extract and a synthetic small molecule prevents rotaviral secretory diarrhoea in neonatal mice. Gut. 2014 Jul;63(7):1120-9. doi: 10.1136/gutjnl-2013-305663. Epub 2013 Sep 19. PubMed PMID: 24052273; PubMed Central PMCID: PMC4048772.
20: Ousingsawat J, Kongsuphol P, Schreiber R, Kunzelmann K. CFTR and TMEM16A are separate but functionally related Cl- channels. Cell Physiol Biochem. 2011;28(4):715-24. doi: 10.1159/000335765. Epub 2011 Dec 14. PubMed PMID: 22178883.
