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執大象，天下往，往而無害，安平泰
WEB: www.eosmedchem.com
EMAIL: info@eosmedchem.com; eosmedchem@gmail.com; eosmedchem@qq.com
TEL: 0086-531-69905422
GMP PLANT: No. 37, Yulong Road, Qufu City, Shandong Province.
1.
Macitentan , CAS# 441798-33-0, White powder, HPLC99.2%, LCMS, HNMR, ROS, MOA, COA is ok, stock more than 100G.
Name: Macitentan
CAS#: 441798-33-0
Chemical Formula: C19H20Br2N6O4S
Exact Mass: 585.96335
Molecular Weight: 588.27
Elemental Analysis: C, 38.79; H, 3.43; Br, 27.17; N, 14.29; O, 10.88; S, 5.45
Synonym: ACT-064992; ACT 064992; ACT064992; Macitentan; brand name: Opsumit.
IUPAC/Chemical Name: N-[5-(4-bromophenyl)-6-{2-[(5-bromopyrimidin-2-yl)oxy]ethoxy}pyrimidin-4-yl]-N'- propylsulfamide
InChi Key: JGCMEBMXRHSZKX-UHFFFAOYSA-N
InChi Code: InChI=1S/C19H20Br2N6O4S/c1-2-7-26-32(28,29)27-17-16(13-3-5-14(20)6-4-13)18(25-12-24-17)30-8-9-31-19-22-10-15(21)11-23-19/h3-6,10-12,26H,2,7-9H2,1H3,(H,24,25,27)
SMILES Code: O=S(NCCC)(NC1=NC=NC(OCCOC2=NC=C(Br)C=N2)=C1C3=CC=C(Br)C=C3)=O
2.
Macitentan intermediates:
Macitentan intermediate, 5-(4-broMophenyl)-4,6-dichloropyriMidine, CAS# 146533-41-7, White powder, HPLC99%, LCMS, HNMR, ROS, MOA, COA is ok, stock more than 1KG.
Macitentan intermediate, N-PropylsulfaMide, CAS# 147962-41-2, White powder, HPLC99%, LCMS, HNMR, ROS, MOA, COA is ok, stock more than 1KG.
Macitentan intermediate, N-Propyl-sulfamide potassium salt, CAS# 1393813-41-6, White powder, HPLC99%, LCMS, HNMR, ROS, MOA, COA is ok, stock more than 1KG.
Macitentan intermediate, N-Propyl-sulfamide sodium salt, CAS# 1642873-03-7, White powder, HPLC99%, LCMS, HNMR, ROS, MOA, COA is ok, stock more than 1KG.
Macitentan intermediate,5-Bromo-2-chloropyrimidine, CAS# 32779-36-5, White powder, HPLC99%, LCMS, HNMR, ROS, MOA, COA is ok, stock more than 1KG.
REFERENCES
1: Shinohara T, Sawada H, Otsuki S, Yodoya N, Kato T, Ohashi H, Zhang E, Saitoh S, Shimpo H, Maruyama K, Komada Y, Mitani Y. Macitentan reverses early obstructive pulmonary vasculopathy in rats: Early intervention in overcoming the survivin-mediated resistance to apoptosis. Am J Physiol Lung Cell Mol Physiol. 2014 Dec 24:ajplung.00129.2014. doi: 10.1152/ajplung.00129.2014. [Epub ahead of print] PubMed PMID: 25539851.
2: Kholdani CA, Fares WH, Trow TK. Macitentan for the treatment of pulmonary arterial hypertension. Vasc Health Risk Manag. 2014 Nov 25;10:665-73. doi: 10.2147/VHRM.S33904. eCollection 2014. PubMed PMID: 25473292; PubMed Central PMCID: PMC4251661.
3: Channick RN, Delcroix M, Ghofrani HA, Hunsche E, Jansa P, Le Brun FO, Mehta S, Pulido T, Rubin LJ, Sastry BK, Simonneau G, Sitbon O, Souza R, Torbicki A, Galiè N. Effect of Macitentan on Hospitalizations: Results From the SERAPHIN Trial (Study with an Endothelin Receptor Antagonist in Pulmonary arterial Hypertension to Improve cliNical outcome). JACC Heart Fail. 2014 Nov 11. pii: S2213-1779(14)00384-9. doi: 10.1016/j.jchf.2014.07.013. [Epub ahead of print] PubMed PMID: 25457902.
4: Tullos NA, Stewart NJ, Davidovich R, Chade AR. Chronic blockade of endothelin A and B receptors using macitentan in experimental renovascular disease. Nephrol Dial Transplant. 2014 Nov 21. pii: gfu361. [Epub ahead of print] PubMed PMID: 25438341.
5: Said K. Macitentan in pulmonary arterial hypertension: The SERAPHIN trial. Glob Cardiol Sci Pract. 2014 Jun 18;2014(2):26-30. doi: 10.5339/gcsp.2014.20. eCollection 2014. PubMed PMID: 25405173; PubMed Central PMCID: PMC4220429.
6: Sood N. Macitentan for the treatment of pulmonary arterial hypertension. Expert Opin Pharmacother. 2014 Dec;15(18):2733-9. doi: 10.1517/14656566.2014.980403. Epub 2014 Nov 11. PubMed PMID: 25385427.
7: Temple IP, Monfredi O, Quigley G, Schneider H, Zi M, Cartwright EJ, Boyett MR, Mahadevan VS, Hart G. Macitentan treatment retards the progression of established pulmonary arterial hypertension in an animal model. Int J Cardiol. 2014 Dec 15;177(2):423-8. doi: 10.1016/j.ijcard.2014.09.005. Epub 2014 Oct 11. PubMed PMID: 25305681; PubMed Central PMCID: PMC4251701.
8: Gatfield J, Mueller Grandjean C, Bur D, Bolli MH, Nayler O. Distinct ETA receptor binding mode of macitentan as determined by site directed mutagenesis. PLoS One. 2014 Sep 16;9(9):e107809. doi: 10.1371/journal.pone.0107809. eCollection 2014. PubMed PMID: 25226600; PubMed Central PMCID: PMC4166607.
9: Kunita-Takanezawa M, Abe K, Hirooka Y, Kuwabara Y, Hirano K, Oka M, Sunagawa K. Novel dual endothelin receptor antagonist macitentan reverses severe pulmonary arterial hypertension in rats. J Cardiovasc Pharmacol. 2014 Nov;64(5):473-80. doi: 10.1097/FJC.0000000000000141. PubMed PMID: 25084082.
10: Dhillon S. Macitentan: a review of its use in patients with pulmonary arterial hypertension. Drugs. 2014 Sep;74(13):1495-507. doi: 10.1007/s40265-014-0266-9. PubMed PMID: 25060980.
11: DuBrock HM, Channick RN. Macitentan for the treatment of pulmonary arterial hypertension. Expert Rev Respir Med. 2014 Aug;8(4):393-9. doi: 10.1586/17476348.2014.937708. Epub 2014 Jul 6. PubMed PMID: 24998329.
12: Spikes L, Williamson T, Satterwhite L. Macitentan for the treatment of pulmonary arterial hypertension. Drugs Today (Barc). 2014 Jun;50(6):401-6. doi: 10.1358/dot.2014.50.6.2146837. Review. PubMed PMID: 24983588.
13: Sidharta PN, van Giersbergen PL, Wolzt M, Dingemanse J. Investigation of mutual pharmacokinetic interactions between macitentan, a novel endothelin receptor antagonist, and sildenafil in healthy subjects. Br J Clin Pharmacol. 2014 Nov;78(5):1035-42. doi: 10.1111/bcp.12447. PubMed PMID: 24962473; PubMed Central PMCID: PMC4243877.
14: Ahn LY, Kim SE, Yi S, Dingemanse J, Lim KS, Jang IJ, Yu KS. Pharmacokinetic-pharmacodynamic relationships of macitentan, a new endothelin receptor antagonist, after multiple dosing in healthy Korean subjects. Am J Cardiovasc Drugs. 2014 Oct;14(5):377-85. doi: 10.1007/s40256-014-0081-4. PubMed PMID: 24906252.
