MedKoo Cat#: 581948 | Name: Trazpiroben

Description:

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

Trazpiroben is a Novel, Potent Dopamine D2/D3 Receptor Antagonist for the Management of Gastroparesis.

Chemical Structure

Trazpiroben
Trazpiroben
CAS#1352993-39-5

Theoretical Analysis

MedKoo Cat#: 581948

Name: Trazpiroben

CAS#: 1352993-39-5

Chemical Formula: C31H39N3O4

Exact Mass: 517.2900

Molecular Weight: 517.67

Elemental Analysis: C, 71.93; H, 7.59; N, 8.12; O, 12.36

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Synonym
Trazpiroben; trazpirobenum; TAK-906; TAK906; TAK 906;
IUPAC/Chemical Name
3-{[1-cyclohexyl-4-oxo-8-(4-oxo-4-phenylbutyl)-1,3,8- triazaspiro[4.5]decan-3-yl]methyl}benzoic acid
InChi Key
BDXJYAAYLZTLEK-UHFFFAOYSA-N
InChi Code
InChI=1S/C31H39N3O4/c35-28(25-10-3-1-4-11-25)15-8-18-32-19-16-31(17-20-32)30(38)33(23-34(31)27-13-5-2-6-14-27)22-24-9-7-12-26(21-24)29(36)37/h1,3-4,7,9-12,21,27H,2,5-6,8,13-20,22-23H2,(H,36,37)
SMILES Code
O=C(O)C1=CC=CC(CN2CN(C3CCCCC3)C4(CCN(CCCC(C5=CC=CC=C5)=O)CC4)C2=O)=C1
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
>3 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

Preparing Stock Solutions

The following data is based on the product molecular weight 517.67 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.

Recalculate based on batch purity %
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
1: Kreckler L, Osinski M, Williams S, Whiting R. Non-Clinical Safety Pharmacology Evaluations of Trazpiroben (TAK-906), a Novel Dopamine D2/D3 Selective Receptor Antagonist for the Management of Gastroparesis. J Exp Pharmacol. 2022 Feb 9;14:43-57. doi: 10.2147/JEP.S332715. PMID: 35173492; PMCID: PMC8842350. 2: Yamaguchi T, Kudou K, Okamoto H, Chen C, Whiting R, Sekino H. Evaluating the Safety, Tolerability, and Disposition of Trazpiroben, a D2 /D3 Receptor Antagonist: Phase I Single- and Multiple-Ascending Dose Studies in Healthy Japanese Participants. Clin Pharmacol Drug Dev. 2021 Dec 29. doi: 10.1002/cpdd.1057. Epub ahead of print. PMID: 34967147. 3: Chen C, Zhang W, Bari M, Almansa C, Baratta M, Rosario M. Evaluation of the Pharmacokinetics of Trazpiroben (TAK-906), a Peripherally Selective D2/D3 Dopamine Receptor Antagonist, in the Presence and Absence of Itraconazole, a Potent CYP 3A4 Inhibitor. Clin Pharmacol. 2021 Jul 12;13:145-155. doi: 10.2147/CPAA.S310609. PMID: 34285598; PMCID: PMC8285519. 4: Whiting RL, Choppin A, Luehr G, Jasper JR. Preclinical Evaluation of the Effects of Trazpiroben (TAK-906), a Novel, Potent Dopamine D2/D3 Receptor Antagonist for the Management of Gastroparesis. J Pharmacol Exp Ther. 2021 Oct;379(1):85-95. doi: 10.1124/jpet.121.000698. Epub 2021 Jul 12. PMID: 34253646. 5: Kuo B, Scimia C, Dukes G, Zhang W, Gupta S, Chen C, Chuang E, Camilleri M. Randomised clinical trial: safety, pharmacokinetics and pharmacodynamics of trazpiroben (TAK-906), a dopamine D2 /D3 receptor antagonist, in patients with gastroparesis. Aliment Pharmacol Ther. 2021 Aug;54(3):267-280. doi: 10.1111/apt.16451. Epub 2021 Jun 20. PMID: 34148244. 6: Nishihara M, Ramsden D, Balani SK. Evaluation of the drug-drug interaction potential for trazpiroben (TAK-906), a D2/D3 receptor antagonist for gastroparesis, towards cytochrome P450s and transporters. Xenobiotica. 2021 Jun;51(6):668-679. doi: 10.1080/00498254.2021.1912438. Epub 2021 Apr 21. PMID: 33879032. 7: Whiting RL, Darpo B, Chen C, Fletcher M, Combs D, Xue H, Stoltz RR. Safety, Pharmacokinetics, and Pharmacodynamics of Trazpiroben (TAK-906), a Novel Selective D2 /D3 Receptor Antagonist: A Phase 1 Randomized, Placebo-Controlled Single- and Multiple-Dose Escalation Study in Healthy Participants. Clin Pharmacol Drug Dev. 2021 Aug;10(8):927-939. doi: 10.1002/cpdd.906. Epub 2021 Jan 18. PMID: 33462988; PMCID: PMC8451790.