Maralixibat Chloride

Catalog No: 25126

CAS Number: 228113-66-4

Purity: 98% Min.

Maralixibat (also known as SHP625, LUM001, and lopixibat) is an ileal bile acid transporter inhibitor, like odevixibat. Maralixibat is indicated for the treatment of cholestatic pruritus in patients with Alagille syndrome, who are at least 1 year old. Previously, patients with cholestatic pruritus associated with Alagille syndrome were treated with antihistamines, rifampin, ursodeoxycholic acid, cholestyramine, naltrexone, and sertraline alone or in combination. Maralixibat represents the first FDA approved treatment for cholestatic pruritus in patients with Alagille syndrome. Maralixibat was granted FDA approval on 29 September 2021.

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Chemical Information

Name	Maralixibat Chloride
Iupac Chemical Name	1-(4-((4-((4R,5R)-3,3-dibutyl-7-(dimethylamino)-4-hydroxy-1,1-dioxido-2,3,4,5-tetrahydrobenzo[b]thiepin-5-yl)phenoxy)methyl)benzyl)-1,4-diazabicyclo[2.2.2]octan-1-ium chloride
Synonyms	LUM-001; LUM 001; LUM001; SHP625; SHP-625; SHP 625; lopixibat; Maralixibat Chloride;
Molecular Formula	C40H56ClN3O4S
Molecular Weight	710.41
Smile	O=S1(C2=CC=C(N(C)C)C=C2[C@@H](C3=CC=C(OCC4=CC=C(C=C4)C[N+]5(CC6)CCN6CC5)C=C3)[C@@H](O)C(CCCC)(CCCC)C1)=O.[Cl-]
InChiKey	POMVPJBWDDJCMP-RUKDTIIFSA-M
InChi	InChI=1S/C40H56N3O4S.ClH/c1-5-7-19-40(20-8-6-2)30-48(45,46)37-18-15-34(41(3)4)27-36(37)38(39(40)44)33-13-16-35(17-14-33)47-29-32-11-9-31(10-12-32)28-43-24-21-42(22-25-43)23-26-43;/h9-18,27,38-39,44H,5-8,19-26,28-30H2,1-4H3;1H/q+1;/p-1/t38-,39-;/m1./s1
CAS Number	228113-66-4
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Formulation	Off-white solid
Purity	98% Min.
Storage	Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years).
Solubility	Soluble in DMSO
Handling
Shipping Condition	Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
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1: Kohut TJ, Gilbert MA, Loomes KM. Alagille Syndrome: A Focused Review on Clinical Features, Genetics, and Treatment. Semin Liver Dis. 2021 Jul 2. doi: 10.1055/s-0041-1730951. Epub ahead of print. PMID: 34215014.

2: Hertel PM, Bull LN, Thompson RJ, Goodrich NP, Ye W, Magee JC, Squires RH, Bass LM, Heubi JE, Kim GE, Ranganathan S, Schwarz KB, Bozic MA, Horslen SP, Clifton MS, Turmelle YP, Suchy FJ, Superina RA, Wang KS, Loomes KM, Kamath BM, Sokol RJ, Shneider BL; Childhood Liver Disease Research Network (ChiLDReN). Mutation Analysis and Disease Features at Presentation in a Multi-Center Cohort of Children With Monogenic Cholestasis. J Pediatr Gastroenterol Nutr. 2021 Aug 1;73(2):169-177. doi: 10.1097/MPG.0000000000003153. PMID: 34016879; PMCID: PMC8373673.

3: Burns J, Davenport M. Adjuvant treatments for biliary atresia. Transl Pediatr. 2020 Jun;9(3):253-265. doi: 10.21037/tp.2016.10.08. PMID: 32775244; PMCID: PMC7347763.

4: Karpen SJ, Kelly D, Mack C, Stein P. Ileal bile acid transporter inhibition as an anticholestatic therapeutic target in biliary atresia and other cholestatic disorders. Hepatol Int. 2020 Sep;14(5):677-689. doi: 10.1007/s12072-020-10070-w. Epub 2020 Jul 11. PMID: 32653991.

5: Kamath BM, Spino C, McLain R, Magee JC, Fredericks EM, Setchell KD, Miethke A, Molleston JP, Mack CL, Squires RH, Alonso EM, Murray KF, Loomes KM, Kyle Jensen M, Karpen SJ, Rosenthal P, Thomas D, Sokol RJ, Shneider BL; Childhood Liver Disease Research Network (ChiLDReN). Unraveling the Relationship Between Itching, Scratch Scales, and Biomarkers in Children With Alagille Syndrome. Hepatol Commun. 2020 May 26;4(7):1012-1018. doi: 10.1002/hep4.1522. PMID: 32626833; PMCID: PMC7327199.

6: Mayo MJ, Pockros PJ, Jones D, Bowlus CL, Levy C, Patanwala I, Bacon B, Luketic V, Vuppalanchi R, Medendorp S, Dorenbaum A, Kennedy C, Novak P, Gu J, Apostol G, Hirschfield GM. A Randomized, Controlled, Phase 2 Study of Maralixibat in the Treatment of Itching Associated With Primary Biliary Cholangitis. Hepatol Commun. 2019 Feb 1;3(3):365-381. doi: 10.1002/hep4.1305. PMID: 30859149; PMCID: PMC6396374.

7: Shneider BL, Spino C, Kamath BM, Magee JC, Bass LM, Setchell KD, Miethke A, Molleston JP, Mack CL, Squires RH, Murray KF, Loomes KM, Rosenthal P, Karpen SJ, Leung DH, Guthery SL, Thomas D, Sherker AH, Sokol RJ; Childhood Liver Disease Research Network. Placebo-Controlled Randomized Trial of an Intestinal Bile Salt Transport Inhibitor for Pruritus in Alagille Syndrome. Hepatol Commun. 2018 Sep 24;2(10):1184-1198. doi: 10.1002/hep4.1244. PMID: 30288474; PMCID: PMC6167076.

8: Malatack JJ, Doyle D. A Drug Regimen for Progressive Familial Cholestasis Type 2. Pediatrics. 2018 Jan;141(1):e20163877. doi: 10.1542/peds.2016-3877. PMID: 29284646.

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25126 - Maralixibat Chloride | CAS 228113-66-4

Maralixibat Chloride

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