Avatrombopag maleate | CAS#677007-74-8 | thrombopoietin receptor agonist

Avatrombopag maleate
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 593081

CAS#: 677007-74-8 (maleate)

Description: Avatrombopag, also known as AKR-501, YM477, AS 1670542 or E5501, is a novel orally-active thrombopoietin (TPO) receptor agonist. AKR-501 specifically targeted the TPO receptor and stimulated megakaryocytopoiesis throughout the development and maturation of megakaryocytes just as rhTPO did. AKR-501 may be useful in the treatment of patients with thrombocytopenia. Avatrombopag was first approved in 2018.

Chemical Structure

Avatrombopag maleate

CAS# 677007-74-8 (maleate)

Instruction

Theoretical Analysis

MedKoo Cat#: 593081
Name: Avatrombopag maleate
CAS#: 677007-74-8 (maleate)
Chemical Formula: C33H38Cl2N6O7S2
Exact Mass: 764.16
Molecular Weight: 765.720
Elemental Analysis: C, 51.76; H, 5.00; Cl, 9.26; N, 10.98; O, 14.63; S, 8.37

Price and Availability

Size	Price	Availability
25mg	USD 250	2 Weeks
50mg	USD 450	2 Weeks
100mg	USD 750	2 Weeks
200mg	USD 1350	2 Weeks
500mg	USD 2850	2 Weeks
1g	USD 3850	2 Weeks
2g	USD 6450	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Related CAS #: 677007-74-8 (maleate) 570406-98-3 (free base)

Synonym: AKR501; AKR 501; AKR-501; YM477; YM-477; YM 477; AS 1670542; AS1670542; AS-1670542; E5501; E-5501; E 5501; Avatrombopag; Avatrombopag maleate.

IUPAC/Chemical Name: 4-Piperidinecarboxylic acid, 1-(3-chloro-5-(((4-(4-chloro-2-thienyl)-5-(4-cyclohexyl-1- piperazinyl)-2-thiazolyl)amino)carbonyl)-2-pyridinyl)-, (2Z)-2-butenedioate (1:1)

InChi Key: MISPBGHDNZYFNM-BTJKTKAUSA-N

InChi Code: InChI=1S/C29H34Cl2N6O3S2.C4H4O4/c30-20-15-23(41-17-20)24-27(37-12-10-35(11-13-37)21-4-2-1-3-5-21)42-29(33-24)34-26(38)19-14-22(31)25(32-16-19)36-8-6-18(7-9-36)28(39)40;5-3(6)1-2-4(7)8/h14-18,21H,1-13H2,(H,39,40)(H,33,34,38);1-2H,(H,5,6)(H,7,8)/b;2-1-

SMILES Code: O=C(C1CCN(C2=NC=C(C(NC3=NC(C4=CC(Cl)=CS4)=C(N5CCN(C6CCCCC6)CC5)S3)=O)C=C2Cl)CC1)O.O=C(O)/C=C\C(O)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

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.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >5 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 765.72 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Mladsi D, Barnett C, Aggarwal K, Vredenburg M, Dieterich D, Kim R. Cost- Effectiveness of Avatrombopag for the Treatment of Thrombocytopenia in Patients with Chronic Liver Disease. Clinicoecon Outcomes Res. 2020 Sep 14;12:515-526. doi: 10.2147/CEOR.S262772. PMID: 32982341; PMCID: PMC7500829.

2: Lim MY, Gilreath JA. Periprocedural use of avatrombopag for neurosurgical interventions: a strategy to avoid platelet utilization. Blood Adv. 2020 Sep 22;4(18):4438-4441. doi: 10.1182/bloodadvances.2020003045. PMID: 32936905; PMCID: PMC7509863.

3: Khemichian S, Terrault NA. Thrombopoietin Receptor Agonists in Patients with Chronic Liver Disease. Semin Thromb Hemost. 2020 Sep;46(6):682-692. doi: 10.1055/s-0040-1715451. Epub 2020 Aug 20. PMID: 32820479.

4: Dieterich DT, Bernstein D, Flamm S, Pockros PJ, Reau N. Review article: a treatment algorithm for patients with chronic liver disease and severe thrombocytopenia undergoing elective medical procedures in the United States. Aliment Pharmacol Ther. 2020 Aug 19. doi: 10.1111/apt.16044. Epub ahead of print. PMID: 32813292.

5: Nilles KM, Flamm SL. Thrombocytopenia in Chronic Liver Disease: New Management Strategies. Clin Liver Dis. 2020 Aug;24(3):437-451. doi: 10.1016/j.cld.2020.04.009. Epub 2020 May 31. PMID: 32620282.

6: Birocchi S, Podda GM, Manzoni M, Casazza G, Cattaneo M. Thrombopoietin receptor agonists for the treatment of primary immune thrombocytopenia: a meta- analysis and systematic review. Platelets. 2020 Apr 12:1-11. doi: 10.1080/09537104.2020.1745168. Epub ahead of print. PMID: 32281449.

7: Saab S, Bernstein D, Hassanein T, Kugelmas M, Kwo P. Treatment Options for Thrombocytopenia in Patients With Chronic Liver Disease Undergoing a Scheduled Procedure. J Clin Gastroenterol. 2020 Jul;54(6):503-511. doi: 10.1097/MCG.0000000000001338. PMID: 32195771.

8: Poordad F, Terrault NA, Alkhouri N, Tian W, Allen LF, Rabinovitz M. Avatrombopag, an Alternate Treatment Option to Reduce Platelet Transfusions in Patients with Thrombocytopenia and Chronic Liver Disease-Integrated Analyses of 2 Phase 3 Studies. Int J Hepatol. 2020 Jan 25;2020:5421632. doi: 10.1155/2020/5421632. PMID: 32047671; PMCID: PMC7003278.

9: Nilles KM, Caldwell SH, Flamm SL. Thrombocytopenia and Procedural Prophylaxis in the Era of Thrombopoietin Receptor Agonists. Hepatol Commun. 2019 Sep 4;3(11):1423-1434. doi: 10.1002/hep4.1423. PMID: 31701067; PMCID: PMC6824078.

10: Abdela J. Current Advance in Thrombopoietin Receptor Agonists in the Management of Thrombocytopenia Associated With Chronic Liver Disease: Focus on Avatrombopag. Clin Med Insights Blood Disord. 2019 Oct 21;12:1179545X19875105. doi: 10.1177/1179545X19875105. Erratum in: Clin Med Insights Blood Disord. 2020 Jan 6;13:1179545X19900859. PMID: 31673229; PMCID: PMC6804364.

11: Hussar DA. New Drugs 2019, part 4. Nursing. 2019 Nov;49(11):34-43. doi: 10.1097/01.NURSE.0000585892.82614.f4. PMID: 31651773.

12: Cheloff AZ, Al-Samkari H. Avatrombopag for the treatment of immune thrombocytopenia and thrombocytopenia of chronic liver disease. J Blood Med. 2019 Sep 5;10:313-321. doi: 10.2147/JBM.S191790. PMID: 31565009; PMCID: PMC6733339.

13: Witkowski M, Witkowska M, Robak T. Autoimmune thrombocytopenia: Current treatment options in adults with a focus on novel drugs. Eur J Haematol. 2019 Dec;103(6):531-541. doi: 10.1111/ejh.13319. Epub 2019 Sep 18. PMID: 31449692.

14: Li C, Li X, Huang F, Yang J, Wu A, Wang L, Qin D, Zou W, Wu J. Efficacy and Safety of Avatrombopag in Patients With Thrombocytopenia: A Systematic Review and Meta-Analysis of Randomized Controlled Trials. Front Pharmacol. 2019 Jul 26;10:829. doi: 10.3389/fphar.2019.00829. PMID: 31402863; PMCID: PMC6677019.

15: Miller JB, Figueroa EJ, Haug RM, Shah NL. Thrombocytopenia in Chronic Liver Disease and the Role of Thrombopoietin Agonists. Gastroenterol Hepatol (N Y). 2019 Jun;15(6):326-332. PMID: 31391802; PMCID: PMC6676354.

16: Xu H, Cai R. Avatrombopag for the treatment of thrombocytopenia in patients with chronic liver disease. Expert Rev Clin Pharmacol. 2019 Sep;12(9):859-865. doi: 10.1080/17512433.2019.1649137. Epub 2019 Aug 5. PMID: 31352834.

17: Hussar DA, Kludjian GA. Prucalopride succinate, Fostamatinib disodium hexahydrate, Avatrombopag maleate, and Lusutrombopag. J Am Pharm Assoc (2003). 2019 Jul-Aug;59(4):601-604. doi: 10.1016/j.japh.2019.05.013. PMID: 31296323.

18: Dou X, Yang R. Current and emerging treatments for immune thrombocytopenia. Expert Rev Hematol. 2019 Sep;12(9):723-732. doi: 10.1080/17474086.2019.1636644. Epub 2019 Jul 4. PMID: 31237783.

19: Clemons Bankston P, Al-Horani RA. New Small Molecule Drugs for Thrombocytopenia: Chemical, Pharmacological, and Therapeutic Use Considerations. Int J Mol Sci. 2019 Jun 20;20(12):3013. doi: 10.3390/ijms20123013. PMID: 31226783; PMCID: PMC6628068.

20: Saab S, Brown RS Jr. Management of Thrombocytopenia in Patients with Chronic Liver Disease. Dig Dis Sci. 2019 Oct;64(10):2757-2768. doi: 10.1007/s10620-019-05615-5. Epub 2019 Apr 22. PMID: 31011942.

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