MedKoo Cat#: 465921 | Name: TASP0277308
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Description:

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

TASP0277308 is a potent and selective sphingosine 1-phosphate 1 (S1P1) receptor antagonist (IC50 = 7.8 nM). TASP0277308 inhibited S1P- as well as VEGF-induced cellular responses, including migration and proliferation of human umbilical vein endothelial cells. Furthermore, TASP0277308 effectively blocked a VEGF-induced tube formation in vitro and significantly suppressed tumor cell-induced angiogenesis in vivo.

Chemical Structure

TASP0277308
TASP0277308
CAS#945725-50-8

Theoretical Analysis

MedKoo Cat#: 465921

Name: TASP0277308

CAS#: 945725-50-8

Chemical Formula: C23H28Cl2N6O3S

Exact Mass: 538.1321

Molecular Weight: 539.48

Elemental Analysis: C, 51.21; H, 5.23; Cl, 13.14; N, 15.58; O, 8.90; S, 5.94

Price and Availability

Size Price Availability Quantity
5mg USD 750.00 2 Weeks
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Related CAS #
No Data
Synonym
TASP0277308; TASP 0277308; TASP-0277308;
IUPAC/Chemical Name
(R)-3,4-dichloro-N-(1-(4-ethyl-5-(3-(4-methylpiperazin-1-yl)phenoxy)-4H-1,2,4-triazol-3-yl)ethyl)benzenesulfonamide
InChi Key
MVOULGOLHZCXLD-MRXNPFEDSA-N
InChi Code
InChI=1S/C23H28Cl2N6O3S/c1-4-31-22(16(2)28-35(32,33)19-8-9-20(24)21(25)15-19)26-27-23(31)34-18-7-5-6-17(14-18)30-12-10-29(3)11-13-30/h5-9,14-16,28H,4,10-13H2,1-3H3/t16-/m1/s1
SMILES Code
O=S(C1=CC=C(Cl)C(Cl)=C1)(N[C@@H](C2=NN=C(OC3=CC=CC(N4CCN(C)CC4)=C3)N2CC)C)=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 539.48 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
Li J, Wang Q, Gao Y, Ma W, Sun Z, Yu Y, Li Y, Li Q, Wang C. Blocking SphK/S1P/S1PR1 axis signaling pathway alleviates remifentanil-induced hyperalgesia in rats. Neurosci Lett. 2023 Mar 28;801:137131. doi: 10.1016/j.neulet.2023.137131. Epub 2023 Feb 15. PMID: 36801239. 1: Chen Z, Doyle TM, Luongo L, Largent-Milnes TM, Giancotti LA, Kolar G, Squillace S, Boccella S, Walker JK, Pendleton A, Spiegel S, Neumann WL, Vanderah TW, Salvemini D. Sphingosine-1-phosphate receptor 1 activation in astrocytes contributes to neuropathic pain. Proc Natl Acad Sci U S A. 2019 May 21;116(21):10557-10562. doi: 10.1073/pnas.1820466116. Epub 2019 May 8. PMID: 31068460; PMCID: PMC6534990. 2: Cuzzocrea S, Doyle T, Campolo M, Paterniti I, Esposito E, Farr SA, Salvemini D. Sphingosine 1-Phosphate Receptor Subtype 1 as a Therapeutic Target for Brain Trauma. J Neurotrauma. 2018 Jul 1;35(13):1452-1466. doi: 10.1089/neu.2017.5391. Epub 2018 Apr 17. PMID: 29310513. 3: Grenald SA, Doyle TM, Zhang H, Slosky LM, Chen Z, Largent-Milnes TM, Spiegel S, Vanderah TW, Salvemini D. Targeting the S1P/S1PR1 axis mitigates cancer- induced bone pain and neuroinflammation. Pain. 2017 Sep;158(9):1733-1742. doi: 10.1097/j.pain.0000000000000965. PMID: 28570482; PMCID: PMC5580091. 4: Fujii Y, Ueda Y, Ohtake H, Ono N, Takayama T, Nakazawa K, Igarashi Y, Goitsuka R. Blocking S1P interaction with S1P₁ receptor by a novel competitive S1P₁-selective antagonist inhibits angiogenesis. Biochem Biophys Res Commun. 2012 Mar 23;419(4):754-60. doi: 10.1016/j.bbrc.2012.02.096. Epub 2012 Feb 24. PMID: 22387544. 5: Fujii Y, Hirayama T, Ohtake H, Ono N, Inoue T, Sakurai T, Takayama T, Matsumoto K, Tsukahara N, Hidano S, Harima N, Nakazawa K, Igarashi Y, Goitsuka R. Amelioration of collagen-induced arthritis by a novel S1P1 antagonist with immunomodulatory activities. J Immunol. 2012 Jan 1;188(1):206-15. doi: 10.4049/jimmunol.1101537. Epub 2011 Nov 30. PMID: 22131329.