Pyr10 | CAS: 1315323-00-2 | TRPC3 Inhibitor

Pyr10
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 564056

CAS#: 1315323-00-2

Description: Pyr10 is a selective inhibitor of the transient receptor potential channel TRPC3.

Chemical Structure

Pyr10

CAS# 1315323-00-2

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 564056
Name: Pyr10
CAS#: 1315323-00-2
Chemical Formula: C18H13F6N3O2S
Exact Mass: 449.06
Molecular Weight: 449.370
Elemental Analysis: C, 48.11; H, 2.92; F, 25.37; N, 9.35; O, 7.12; S, 7.13

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 270
25mg	USD 640
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: Pyr10; Pyr-10; Pyr 10

IUPAC/Chemical Name: N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-4-methyl-benzenesulfonamide

InChi Key: CVALMMCIOLXHDM-UHFFFAOYSA-N

InChi Code: InChI=1S/C18H13F6N3O2S/c1-11-2-8-14(9-3-11)30(28,29)26-12-4-6-13(7-5-12)27-16(18(22,23)24)10-15(25-27)17(19,20)21/h2-10,26H,1H3

SMILES Code: O=S(C1=CC=C(C)C=C1)(NC2=CC=C(N3N=C(C(F)(F)F)C=C3C(F)(F)F)C=C2)=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: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in ethanol

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.03.00

More Info:

Product Data:

Product Data

Instruction:

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Biological target:	Pyr10 is a TRPC3 channel inhibitor (IC50 = 0.72 μM for TRPC3 mediated calcium entry in vitro), which displays approximately 18-fold selectivity for TRPC3-mediated receptor operated calcium entry (ROCE) over STIM1/Orai1-mediated store operated calcium entry (SOCE). Pyr10 inhibits NFATc3 activation and inhibits proliferation of rat ventricular cardiac fibroblasts.
In vitro activity:	The in vitro activity of pyr10, a pyrazole derivative, was investigated in this study using cloned human TWIK-related K+ channels (TREKs) and TWIK-related acid-sensitive K+ channel 2 (TASK-2) channels expressed in HEK293T cells. Pyr10 exhibited subtype-specific inhibition, primarily targeting ITREK1, while sparing ITREK2. Pyr10 displayed inhibitory effects on ITASK2. At a concentration of 100μM, pyr10 resulted in a 70.9±3.1% reduction in ITASK2 current. Reference: Eur J Pharmacol. 2016 Nov 15;791:686-695. https://pubmed.ncbi.nlm.nih.gov/27568832/
In vivo activity:	PYR10 significantly reduced bladder excitability in detrusor overactive and control rats, but the decrease of the bladder excitability of detrusor overactivity rats was more obvious. PYR10 significantly reduced the intracellular calcium concentration in smooth muscle cells in detrusor overactivity and control rats. Reference: Lab Invest. 2022 Jan;102(1):48-56. https://pubmed.ncbi.nlm.nih.gov/34497367/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	Ethanol	44.9	100.00

Preparing Stock Solutions

The following data is based on the product molecular weight 449.37 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:	1. Kim HJ, Woo J, Nam Y, Nam JH, Kim WK. Differential modulation of TWIK-related K+ channel (TREK) and TWIK-related acid-sensitive K+ channel 2 (TASK2) activity by pyrazole compounds. Eur J Pharmacol. 2016 Nov 15;791:686-695. doi: 10.1016/j.ejphar.2016.08.030. Epub 2016 Aug 26. PMID: 27568832. 2. Schleifer H, Doleschal B, Lichtenegger M, Oppenrieder R, Derler I, Frischauf I, Glasnov TN, Kappe CO, Romanin C, Groschner K. Novel pyrazole compounds for pharmacological discrimination between receptor-operated and store-operated Ca(2+) entry pathways. Br J Pharmacol. 2012 Dec;167(8):1712-22. doi: 10.1111/j.1476-5381.2012.02126.x. PMID: 22862290; PMCID: PMC3525873. 3. Zhu J, Fan Y, Lu Q, Yang Y, Li H, Liu X, Zhang H, Sun B, Liu Q, Zhao J, Yang Z, Li L, Feng H, Xu J. Increased transient receptor potential canonical 3 activity is involved in the pathogenesis of detrusor overactivity by dynamic interaction with Na+/Ca2+ exchanger 1. Lab Invest. 2022 Jan;102(1):48-56. doi: 10.1038/s41374-021-00665-8. Epub 2021 Sep 8. PMID: 34497367. 4. Saliba Y, Jebara V, Hajal J, Maroun R, Chacar S, Smayra V, Abramowitz J, Birnbaumer L, Farès N. Transient Receptor Potential Canonical 3 and Nuclear Factor of Activated T Cells C3 Signaling Pathway Critically Regulates Myocardial Fibrosis. Antioxid Redox Signal. 2019 Jun 1;30(16):1851-1879. doi: 10.1089/ars.2018.7545. Epub 2018 Nov 29. PMID: 30318928; PMCID: PMC6486676.
In vitro protocol:	1. Kim HJ, Woo J, Nam Y, Nam JH, Kim WK. Differential modulation of TWIK-related K+ channel (TREK) and TWIK-related acid-sensitive K+ channel 2 (TASK2) activity by pyrazole compounds. Eur J Pharmacol. 2016 Nov 15;791:686-695. doi: 10.1016/j.ejphar.2016.08.030. Epub 2016 Aug 26. PMID: 27568832. 2. Schleifer H, Doleschal B, Lichtenegger M, Oppenrieder R, Derler I, Frischauf I, Glasnov TN, Kappe CO, Romanin C, Groschner K. Novel pyrazole compounds for pharmacological discrimination between receptor-operated and store-operated Ca(2+) entry pathways. Br J Pharmacol. 2012 Dec;167(8):1712-22. doi: 10.1111/j.1476-5381.2012.02126.x. PMID: 22862290; PMCID: PMC3525873.
In vivo protocol:	1. Zhu J, Fan Y, Lu Q, Yang Y, Li H, Liu X, Zhang H, Sun B, Liu Q, Zhao J, Yang Z, Li L, Feng H, Xu J. Increased transient receptor potential canonical 3 activity is involved in the pathogenesis of detrusor overactivity by dynamic interaction with Na+/Ca2+ exchanger 1. Lab Invest. 2022 Jan;102(1):48-56. doi: 10.1038/s41374-021-00665-8. Epub 2021 Sep 8. PMID: 34497367. 2. Saliba Y, Jebara V, Hajal J, Maroun R, Chacar S, Smayra V, Abramowitz J, Birnbaumer L, Farès N. Transient Receptor Potential Canonical 3 and Nuclear Factor of Activated T Cells C3 Signaling Pathway Critically Regulates Myocardial Fibrosis. Antioxid Redox Signal. 2019 Jun 1;30(16):1851-1879. doi: 10.1089/ars.2018.7545. Epub 2018 Nov 29. PMID: 30318928; PMCID: PMC6486676.

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1: Chauvet S, Jarvis L, Chevallet M, Shrestha N, Groschner K, Bouron A. Pharmacological Characterization of the Native Store-Operated Calcium Channels of Cortical Neurons from Embryonic Mouse Brain. Front Pharmacol. 2016 Dec 12;7:486. doi: 10.3389/fphar.2016.00486. eCollection 2016. Erratum in: Front Pharmacol. 2017 Mar 22;8:152. PubMed PMID: 28018223; PubMed Central PMCID: PMC5149554.

2: Álvarez-Miguel I, Cidad P, Pérez-García MT, López-López JR. Differences in TRPC3 and TRPC6 channels assembly in mesenteric vascular smooth muscle cells in essential hypertension. J Physiol. 2017 Mar 1;595(5):1497-1513. doi: 10.1113/JP273327. Epub 2016 Dec 29. PubMed PMID: 27861908; PubMed Central PMCID: PMC5330869.

3: Alkhani H, Ase AR, Grant R, O'Donnell D, Groschner K, Séguéla P. Contribution of TRPC3 to store-operated calcium entry and inflammatory transductions in primary nociceptors. Mol Pain. 2014 Jun 26;10:43. doi: 10.1186/1744-8069-10-43. PubMed PMID: 24965271; PubMed Central PMCID: PMC4118315.

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