MedKoo Cat#: 464264 | Name: TAS 205
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Description:

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

TAS 205 is an inhibitor of hematopoietic prostaglandin D synthase (H-PGDS; IC50 = 55.8 nM). It is selective for H-PGDS over lipocalin-type PGDS (L-PGDS) at 100 µM, as well as over enzyme and receptor panels at 10 µM. TAS 205 inhibits production of prostaglandin D2 (PGD2) induced by A23187 in KU812 human and RBL-2H3 rat basophils with IC50 values of 78.3 and 181.3 nM, respectively. It inhibits ovalbumin-induced nasal lavage fluid eosinophil infiltration and late-phase nasal obstruction in an ovalbumin-sensitized guinea pig model of allergic rhinitis when administered at a dose of 30 mg/kg.

Chemical Structure

TAS 205
TAS 205
CAS#1584160-52-0

Theoretical Analysis

MedKoo Cat#: 464264

Name: TAS 205

CAS#: 1584160-52-0

Chemical Formula: C27H38N6O5

Exact Mass: 526.2904

Molecular Weight: 526.64

Elemental Analysis: C, 61.58; H, 7.27; N, 15.96; O, 15.19

Price and Availability

Size Price Availability Quantity
1mg USD 350.00 2 Weeks
5mg USD 950.00 2 Weeks
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Related CAS #
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Synonym
TAS 205; TAS205; TAS-205;
IUPAC/Chemical Name
4-(1-methyl-1H-pyrrole-2-carbonyl)-N-(4-(4-(morpholine-4-carbonyl)piperidin-1-yl)phenyl)piperazine-1-carboxamide hydrate
InChi Key
NFXCKTKGAJDCBA-UHFFFAOYSA-N
InChi Code
InChI=1S/C27H36N6O4.H2O/c1-29-10-2-3-24(29)26(35)31-13-15-33(16-14-31)27(36)28-22-4-6-23(7-5-22)30-11-8-21(9-12-30)25(34)32-17-19-37-20-18-32;/h2-7,10,21H,8-9,11-20H2,1H3,(H,28,36);1H2
SMILES Code
O=C(NC1=CC=C(C=C1)N2CCC(C(N3CCOCC3)=O)CC2)N4CCN(C(C5=CC=CN5C)=O)CC4.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
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

Preparing Stock Solutions

The following data is based on the product molecular weight 526.64 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: Osawa H, Kurohara T, Ito T, Shibata N, Demizu Y. CRBN ligand expansion for hematopoietic prostaglandin D2 synthase (H-PGDS) targeting PROTAC design and their in vitro ADME profiles. Bioorg Med Chem. 2023 Apr 15;84:117259. doi: 10.1016/j.bmc.2023.117259. Epub 2023 Mar 30. PMID: 37018877. 2: Murakami Y, Osawa H, Kurohara T, Yanase Y, Ito T, Yokoo H, Shibata N, Naito M, Aritake K, Demizu Y. Structure-activity relationship study of PROTACs against hematopoietic prostaglandin D2 synthase. RSC Med Chem. 2022 Sep 23;13(12):1495-1503. doi: 10.1039/d2md00284a. PMID: 36561070; PMCID: PMC9749925. 3: Kracht KD, Eichorn NL, Berlau DJ. Perspectives on the advances in the pharmacotherapeutic management of Duchenne muscular dystrophy. Expert Opin Pharmacother. 2022 Oct;23(15):1701-1710. doi: 10.1080/14656566.2022.2130246. Epub 2022 Oct 3. PMID: 36168943. 4: Ferizovic N, Summers J, de Zárate IBO, Werner C, Jiang J, Landfeldt E, Buesch K. Prognostic indicators of disease progression in Duchenne muscular dystrophy: A literature review and evidence synthesis. PLoS One. 2022 Mar 25;17(3):e0265879. doi: 10.1371/journal.pone.0265879. PMID: 35333888; PMCID: PMC8956179. 5: Aoyagi H, Kajiwara D, Tsunekuni K, Tanaka K, Miyoshi K, Hirasawa N. Potential synergistic effects of novel hematopoietic prostaglandin D synthase inhibitor TAS-205 and different types of anti-allergic medicine on nasal obstruction in a Guinea pig model of experimental allergic rhinitis. Eur J Pharmacol. 2020 May 15;875:173030. doi: 10.1016/j.ejphar.2020.173030. Epub 2020 Feb 19. PMID: 32084417. 6: Komaki H, Maegaki Y, Matsumura T, Shiraishi K, Awano H, Nakamura A, Kinoshita S, Ogata K, Ishigaki K, Saitoh S, Funato M, Kuru S, Nakayama T, Iwata Y, Yajima H, Takeda S. Early phase 2 trial of TAS-205 in patients with Duchenne muscular dystrophy. Ann Clin Transl Neurol. 2020 Feb;7(2):181-190. doi: 10.1002/acn3.50978. Epub 2020 Jan 20. PMID: 31957953; PMCID: PMC7034509. 7: Takeshita E, Komaki H, Shimizu-Motohashi Y, Ishiyama A, Sasaki M, Takeda S. A phase I study of TAS-205 in patients with Duchenne muscular dystrophy. Ann Clin Transl Neurol. 2018 Oct 10;5(11):1338-1349. doi: 10.1002/acn3.651. PMID: 30480028; PMCID: PMC6243382.