YM-58483
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 555214

CAS#: 223499-30-7

Description: YM-58483, also known as BTP 2, is a potent inhibitor of CRAC channels, blocking thapsigargin-induced sustained calcium influx, Th2 cytokine production, and NF-AT-driven promoter activity in T lymphocytes (IC50 = 100 nM).


Price and Availability

Size
Price

50mg
USD 450
500mg
USD 2150
5g
USD 8650
Size
Price

100mg
USD 750
1g
USD 3450
Size
Price

200mg
USD 1250
2g
USD 4650

YM-58483, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 555214
Name: YM-58483
CAS#: 223499-30-7
Chemical Formula: C15H9F6N5OS
Exact Mass: 421.0432
Molecular Weight: 421.3214
Elemental Analysis: C, 42.76; H, 2.15; F, 27.06; N, 16.62; O, 3.80; S, 7.61


Synonym: YM-58483; YM 58483; YM58483; BTP 2; BTP-2; BTP2.

IUPAC/Chemical Name: N-[4-[3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-4-methyl-1,2,3-thiadiazole-5-carboxamide

InChi Key: XPRZIORDEVHURQ-UHFFFAOYSA-N

InChi Code: InChI=1S/C15H9F6N5OS/c1-7-12(28-25-23-7)13(27)22-8-2-4-9(5-3-8)26-11(15(19,20)21)6-10(24-26)14(16,17)18/h2-6H,1H3,(H,22,27)

SMILES Code: O=C(C1=C(C)N=NS1)NC2=CC=C(N3N=C(C(F)(F)F)C=C3C(F)(F)F)C=C2


Technical Data

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:
>2 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).

Harmonized System Code:
293490


References

1: Miyoshi M, Liu S, Morizane A, Takemasa E, Suzuki Y, Kiyoi T, Maeyama K, Mogi M. Efficacy of constant long-term delivery of YM-58483 for the treatment of rheumatoid arthritis. Eur J Pharmacol. 2018 Apr 5;824:89-98. doi: 10.1016/j.ejphar.2018.02.006. Epub 2018 Feb 8. PubMed PMID: 29428471.

2: Domenichini F, Terrié E, Arnault P, Harnois T, Magaud C, Bois P, Constantin B, Coronas V. Store-Operated Calcium Entries Control Neural Stem Cell Self-Renewal in the Adult Brain Subventricular Zone. Stem Cells. 2018 Jan 23. doi: 10.1002/stem.2786. [Epub ahead of print] PubMed PMID: 29359518.

3: Wei D, Mei Y, Xia J, Hu H. Orai1 and Orai3 Mediate Store-Operated Calcium Entry Contributing to Neuronal Excitability in Dorsal Root Ganglion Neurons. Front Cell Neurosci. 2017 Dec 19;11:400. doi: 10.3389/fncel.2017.00400. eCollection 2017. PubMed PMID: 29311831; PubMed Central PMCID: PMC5742109.

4: González-Sánchez P, Del Arco A, Esteban JA, Satrústegui J. Store-Operated Calcium Entry Is Required for mGluR-Dependent Long Term Depression in Cortical Neurons. Front Cell Neurosci. 2017 Dec 14;11:363. doi: 10.3389/fncel.2017.00363. eCollection 2017. PubMed PMID: 29311823; PubMed Central PMCID: PMC5735122.

5: Salker MS, Singh Y, Durairaj RRP, Yan J, Alauddin M, Zeng N, Steel JH, Zhang S, Nautiyal J, Webster Z, Brucker SY, Wallwiener D, Anne Croy B, Brosens JJ, Lang F. LEFTY2 inhibits endometrial receptivity by downregulating Orai1 expression and store-operated Ca(2+) entry. J Mol Med (Berl). 2018 Feb;96(2):173-182. doi: 10.1007/s00109-017-1610-9. Epub 2017 Dec 11. PubMed PMID: 29230527; PubMed Central PMCID: PMC5778154.

6: Liu S, Hasegawa H, Takemasa E, Suzuki Y, Oka K, Kiyoi T, Takeda H, Ogasawara T, Sawasaki T, Yasukawa M, Maeyama K. Efficiency and Safety of CRAC Inhibitors in Human Rheumatoid Arthritis Xenograft Models. J Immunol. 2017 Sep 1;199(5):1584-1595. doi: 10.4049/jimmunol.1700192. Epub 2017 Jul 17. PubMed PMID: 28716825.

7: Dart AE, Worth DC, Muir G, Chandra A, Morris JD, McKee C, Verrill C, Bryant RJ, Gordon-Weeks PR. The drebrin/EB3 pathway drives invasive activity in prostate cancer. Oncogene. 2017 Jul 20;36(29):4111-4123. doi: 10.1038/onc.2017.45. Epub 2017 Mar 20. PubMed PMID: 28319065; PubMed Central PMCID: PMC5537610.

8: Zhang W, Qi Z, Wang Y. BTP2, a Store-Operated Calcium Channel Inhibitor, Attenuates Lung Ischemia-Reperfusion Injury in Rats. Inflammation. 2017 Jun;40(3):778-787. doi: 10.1007/s10753-017-0522-8. PubMed PMID: 28168659.

9: Souza Bomfim GH, Mendez-Lopez I, Arranz-Tagarro JA, Ferraz Carbonel AA, Roman-Campos D, Padín JF, Garcia AG, Jurkiewicz A, Jurkiewicz NH. Functional Upregulation of STIM-1/Orai-1-Mediated Store-Operated Ca2+ Contributing to the Hypertension Development Elicited by Chronic EtOH Consumption. Curr Vasc Pharmacol. 2017;15(3):265-281. doi: 10.2174/1570161115666170201122750. PubMed PMID: 28155613.

10: Wang J, Hogan JO, Kim D. Voltage- and receptor-mediated activation of a non-selective cation channel in rat carotid body glomus cells. Respir Physiol Neurobiol. 2017 Mar;237:13-21. doi: 10.1016/j.resp.2016.12.005. Epub 2016 Dec 21. PubMed PMID: 28013061; PubMed Central PMCID: PMC5272830.

11: Wu YL, Xie J, An SW, Oliver N, Barrezueta NX, Lin MH, Birnbaumer L, Huang CL. Inhibition of TRPC6 channels ameliorates renal fibrosis and contributes to renal protection by soluble klotho. Kidney Int. 2017 Apr;91(4):830-841. doi: 10.1016/j.kint.2016.09.039. Epub 2016 Dec 12. PubMed PMID: 27979597; PubMed Central PMCID: PMC5357448.

12: Chan CM, Huang DY, Huang YP, Hsu SH, Kang LY, Shen CM, Lin WW. Methylglyoxal induces cell death through endoplasmic reticulum stress-associated ROS production and mitochondrial dysfunction. J Cell Mol Med. 2016 Sep;20(9):1749-60. doi: 10.1111/jcmm.12893. Epub 2016 Jun 16. PubMed PMID: 27307396; PubMed Central PMCID: PMC4988286.

13: Gao X, Xia J, Munoz FM, Manners MT, Pan R, Meucci O, Dai Y, Hu H. STIMs and Orai1 regulate cytokine production in spinal astrocytes. J Neuroinflammation. 2016 May 31;13(1):126. doi: 10.1186/s12974-016-0594-7. PubMed PMID: 27245842; PubMed Central PMCID: PMC4886427.

14: Sabourin J, Bartoli F, Antigny F, Gomez AM, Benitah JP. Transient Receptor Potential Canonical (TRPC)/Orai1-dependent Store-operated Ca2+ Channels: NEW TARGETS OF ALDOSTERONE IN CARDIOMYOCYTES. J Biol Chem. 2016 Jun 17;291(25):13394-409. doi: 10.1074/jbc.M115.693911. Epub 2016 Apr 22. PubMed PMID: 27129253; PubMed Central PMCID: PMC4933247.

15: Nguyen TM, Duittoz A, Praud C, Combarnous Y, Blesbois E. Calcium channels in chicken sperm regulate motility and the acrosome reaction. FEBS J. 2016 May;283(10):1902-20. doi: 10.1111/febs.13710. Epub 2016 Apr 13. PubMed PMID: 26990886.

16: Munoz F, Hu H. The Role of Store-operated Calcium Channels in Pain. Adv Pharmacol. 2016;75:139-51. doi: 10.1016/bs.apha.2015.12.005. Epub 2016 Jan 27. Review. PubMed PMID: 26920011.

17: Zuccolo E, Bottino C, Diofano F, Poletto V, Codazzi AC, Mannarino S, Campanelli R, Fois G, Marseglia GL, Guerra G, Montagna D, Laforenza U, Rosti V, Massa M, Moccia F. Constitutive Store-Operated Ca(2+) Entry Leads to Enhanced Nitric Oxide Production and Proliferation in Infantile Hemangioma-Derived Endothelial Colony-Forming Cells. Stem Cells Dev. 2016 Feb 15;25(4):301-19. doi: 10.1089/scd.2015.0240. Epub 2016 Jan 26. PubMed PMID: 26654173.

18: Zhong W, Chebolu S, Darmani NA. Thapsigargin-induced activation of Ca(2+)-CaMKII-ERK in brainstem contributes to substance P release and induction of emesis in the least shrew. Neuropharmacology. 2016 Apr;103:195-210. doi: 10.1016/j.neuropharm.2015.11.023. Epub 2015 Nov 26. PubMed PMID: 26631534.

19: Qi Z, Wang Y, Zhou H, Liang N, Yang L, Liu L, Zhang W. The Central Analgesic Mechanism of YM-58483 in Attenuating Neuropathic Pain in Rats. Cell Mol Neurobiol. 2016 Oct;36(7):1035-43. doi: 10.1007/s10571-015-0292-5. Epub 2015 Oct 29. PubMed PMID: 26514127.

20: Gao XH, Gao R, Tian YZ, McGonigle P, Barrett JE, Dai Y, Hu H. A store-operated calcium channel inhibitor attenuates collagen-induced arthritis. Br J Pharmacol. 2015 Jun;172(12):2991-3002. doi: 10.1111/bph.13104. Epub 2015 Mar 27. PubMed PMID: 25651822; PubMed Central PMCID: PMC4459018.