WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H130445
CAS#: N/A
Description: TP0473292 is an adamantane carboxylic acid ester prodrug of TP0178894, a metabotropic glutamate 2 and 3 receptor antagonist for use as an antidepressant. TP0473292 has undergone phase 1 clinical trials for treatment of depression.
Hodoodo Cat#: H130445
Name: TP0473292
CAS#: N/A
Chemical Formula: C28H33F2NO7
Exact Mass: 533.22
Molecular Weight: 533.570
Elemental Analysis: C, 63.03; H, 6.23; F, 7.12; N, 2.63; O, 20.99
This product is not in stock, which may be available by custom synthesis.
For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge).
Quote less than 1g will not be provided. To request quote, please email to sales @hodoodo.com or click below button.
Note: Price will be listed if it is available in the future.
Synonym: TP0473292; TP 0473292; TP-0473292
IUPAC/Chemical Name: (1R,2R,3R,5R,6R)-2-(((S)-1-((adamantane-1-carbonyl)oxy)ethoxy)carbonyl)-2-amino-6-fluoro-3-((4-fluorobenzyl)oxy)bicyclo[3.1.0]hexane-6-carboxylic acid
InChi Key: OCKJWSRXCCMMEI-AHGQKZNCSA-N
InChi Code: InChI=1S/C28H33F2NO7/c1-14(37-24(34)26-10-16-6-17(11-26)8-18(7-16)12-26)38-25(35)28(31)21(9-20-22(28)27(20,30)23(32)33)36-13-15-2-4-19(29)5-3-15/h2-5,14,16-18,20-22H,6-13,31H2,1H3,(H,32,33)/t14-,16?,17?,18?,20+,21+,22-,26?,27+,28-/m0/s1
SMILES Code: O=C([C@@]1(F)[C@]2([H])C[C@@H](OCC3=CC=C(F)C=C3)[C@@](N)(C(O[C@H](OC(C45CC6CC(C5)CC(C6)C4)=O)C)=O)[C@]12[H])O
Appearance: To be determined
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: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
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:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 533.57 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. Inatani S, Ochi M, Kinoshita K, Yamaguchi JI, Endo H. Preclinical metabolism and disposition of TP0473292, a novel oral prodrug of the potent metabotropic glutamate 2/3 receptor antagonist TP0178894 for the treatment of depression. Drug Metab Dispos. 2023 Feb 8:DMD-AR-2022-001116. doi: 10.1124/dmd.122.001116. Epub ahead of print. PMID: 36754836.
2. Watanabe M, Marcy B, Hiroki A, Watase H, Kinoshita K, Iijima M, Marumo T, Zarate CA, Chaki S. Evaluation of the Safety, Tolerability, and Pharmacokinetic Profiles of TP0473292 (TS-161), A Prodrug of a Novel Orthosteric mGlu2/3 Receptor Antagonist TP0178894, in Healthy Subjects and Its Antidepressant-Like Effects in Rodents. Int J Neuropsychopharmacol. 2022 Feb 11;25(2):106-117. doi: 10.1093/ijnp/pyab062. PMID: 34534292; PMCID: PMC8832229.