WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H201741
CAS#: 851606-62-7 (choline)
Description: Totrombopag, also known LGD-4665, GSK2285921 and SB559448, is an oral thromobopoietin receptor agonist, is being developed as a new generation small molecule thrombopoietin (TPO) mimetic. It is a highly selective and potent agonist of the TPO receptor and therefore induces differentiation and proliferation of megakaryocytes. The pharmacologic characteristics indicate potential therapeutic use in thrombocytopenic patients with a variety of clinical etiologies.
Hodoodo Cat#: H201741
Name: Totrombopag choline
CAS#: 851606-62-7 (choline)
Chemical Formula: C30H35N9O3
Exact Mass: 0.00
Molecular Weight: 569.670
Elemental Analysis: C, 63.25; H, 6.19; N, 22.13; O, 8.43
Related CAS #: 376592-42-6 (free base) 851606-62-7 (choline)
Synonym: SB559448; SB 559448; SB-559448; LGD-4665; LGD4665; LGD 4665; GSK2285921; GSK-2285921; GSK 2285921; C116875; Totrombopag choline
IUPAC/Chemical Name: 2-hydroxy-N,N,N-trimethylethan-1-aminium (E)-5-(3'-((1-(3,4-dimethylphenyl)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-4-yl)diazenyl)-2'-hydroxy-[1,1'-biphenyl]-3-yl)tetrazol-1-ide
InChi Key: JKVHRBKMPPIUNC-UHFFFAOYSA-N
InChi Code: InChI=1S/C25H21N8O2.C5H14NO/c1-14-10-11-19(12-15(14)2)33-25(35)22(16(3)30-33)27-26-21-9-5-8-20(23(21)34)17-6-4-7-18(13-17)24-28-31-32-29-24;1-6(2,3)4-5-7/h4-13,22H,1-3H3,(H-,27,28,29,31,32,34);7H,4-5H2,1-3H3/q-1;+1
SMILES Code: C[N+](C)(C)CCO.OC1=C(/N=N/C2C(C)=NN(C3=CC=C(C)C(C)=C3)C2=O)C=CC=C1C4=CC=CC(C5=NN=N[N-]5)=C4
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, not soluble in water.
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: Related CAS# 376592-42-6 (Totrombopag) 851606-62-7 (Totrombopag choline)
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 569.67 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: |
1. Fox, Norma E.; Lim, Jihyang; Chen, Rose; Geddis, Amy E. F104S c-Mpl responds to a transmembrane domain-binding thrombopoietin receptor agonist: Proof of concept that selected receptor mutations in congenital amegakaryocytic thrombocytopenia can be stimulated with alternative thrombopoietic agents. Experimental Hematology (New York, NY, United States) (2010), 38(5), 384-391.
2. Rice, Lawrence. Treatment of immune thrombocytopenic purpura: focus on eltrombopag. Biologics: Targets & Therapy (2009), 3 151-157.
3. Tomillero A; Moral M A Gateways to clinical trials. Methods and findings in experimental and clinical pharmacology (2008), 30(7), 543-88.
4. Bayes M; Rabasseda X Gateways to clinical trials. Methods and findings in experimental and clinical pharmacology (2008), 30(1), 67-99.