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MedKoo Cat#: 530945 | Name: SAR-7334 HCl
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Description:

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

SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels that opens new opportunities for the investigation of TRPC channel function in vivo. SAR7334 inhibited TRPC6, TRPC3 and TRPC7-mediated Ca(2+) influx into cells with IC50 s of 9.5, 282 and 226 nM, whereas TRPC4 and TRPC5-mediated Ca(2+) entry was not affected.

Chemical Structure

SAR-7334 HCl
SAR-7334 HCl
CAS#1333207-63-8 (HCl)

Theoretical Analysis

MedKoo Cat#: 530945

Name: SAR-7334 HCl

CAS#: 1333207-63-8 (HCl)

Chemical Formula: C21H24Cl3N3O

Exact Mass: 0.0000

Molecular Weight: 440.79

Elemental Analysis: C, 57.22; H, 5.49; Cl, 24.13; N, 9.53; O, 3.63

Price and Availability

Size Price Availability Quantity
10mg USD 750.00
50mg USD 1,250.00
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Related CAS #
1333210-07-3 (free base) 1333207-63-8 (HCl)
Synonym
SAR-7334; SAR 7334; SAR7334. SAR-7334 HCl, SAR-7334 hydrochloride
IUPAC/Chemical Name
4-[[(1R,2R)-2-[(3R)-3-Amino-1-piperidinyl]-2,3-dihydro-1H-inden-1-yl]oxy]-3-chlorobenzonitrile dihydrochloride
InChi Key
LFMYIKNZNTZSJX-IQJQELQDSA-N
InChi Code
InChI=1S/C21H22ClN3O.2ClH/c22-18-10-14(12-23)7-8-20(18)26-21-17-6-2-1-4-15(17)11-19(21)25-9-3-5-16(24)13-25;;/h1-2,4,6-8,10,16,19,21H,3,5,9,11,13,24H2;2*1H/t16-,19-,21-;;/m1../s1
SMILES Code
N#CC1=CC=C(O[C@H]2[C@H](N3C[C@H](N)CCC3)CC4=C2C=CC=C4)C(Cl)=C1.[H]Cl.[H]Cl
Appearance
Solid powder
Purity
>95% (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).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
SAR-7334 HCl inhibits TRPC6 currents with a IC50 value of 7.9 nM.
In vitro activity:
RYR1-p.G2435R mouse muscle cells displayed persistently elevated intracellular calcium and sodium levels, particularly in homozygotes, when exposed to a TRPC3/6 activator, 1-oleoyl-2-acetyl-sn-glycerol. SAR-7334 blocked elevated calcium/sodium levels and removed extracellular calcium. Local pre-treatment with SAR-7334 mitigated the rise in intracellular calcium observed in RYR1-p.G2435R muscles during halothane exposure. Reference: Anesthesiology. 2020 Aug;133(2):364-376. https://pubmed.ncbi.nlm.nih.gov/32665491/
In vivo activity:
In an initial short-term study, SAR-7334 did not change mean arterial pressure in spontaneously hypertensive rats, suggesting that it may have cardiovascular safety and long-term use potential. Reference: Br J Pharmacol. 2015 Jul;172(14):3650-60. https://pubmed.ncbi.nlm.nih.gov/25847402/
Solvent mg/mL mM
Solubility
DMSO 100.0 226.87
Water 50.0 113.43
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 440.79 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
Formulation protocol:
1. Rafael Lopez J, Kaura V, Hopkins P, Liu X, Uryach A, Adams J, Allen PD. Transient Receptor Potential Cation Channels and Calcium Dyshomeostasis in a Mouse Model Relevant to Malignant Hyperthermia. Anesthesiology. 2020 Aug;133(2):364-376. doi: 10.1097/ALN.0000000000003387. PMID: 32665491; PMCID: PMC7367496. 2. Lopez JR, Uryash A, Faury G, Estève E, Adams JA. Contribution of TRPC Channels to Intracellular Ca2 + Dyshomeostasis in Smooth Muscle From mdx Mice. Front Physiol. 2020 Feb 20;11:126. doi: 10.3389/fphys.2020.00126. PMID: 32153426; PMCID: PMC7044154. 3. Maier T, Follmann M, Hessler G, Kleemann HW, Hachtel S, Fuchs B, Weissmann N, Linz W, Schmidt T, Löhn M, Schroeter K, Wang L, Rütten H, Strübing C. Discovery and pharmacological characterization of a novel potent inhibitor of diacylglycerol-sensitive TRPC cation channels. Br J Pharmacol. 2015 Jul;172(14):3650-60. doi: 10.1111/bph.13151. Epub 2015 May 19. PMID: 25847402; PMCID: PMC4507166.
In vitro protocol:
1. Rafael Lopez J, Kaura V, Hopkins P, Liu X, Uryach A, Adams J, Allen PD. Transient Receptor Potential Cation Channels and Calcium Dyshomeostasis in a Mouse Model Relevant to Malignant Hyperthermia. Anesthesiology. 2020 Aug;133(2):364-376. doi: 10.1097/ALN.0000000000003387. PMID: 32665491; PMCID: PMC7367496. 2. Lopez JR, Uryash A, Faury G, Estève E, Adams JA. Contribution of TRPC Channels to Intracellular Ca2 + Dyshomeostasis in Smooth Muscle From mdx Mice. Front Physiol. 2020 Feb 20;11:126. doi: 10.3389/fphys.2020.00126. PMID: 32153426; PMCID: PMC7044154.
In vivo protocol:
1. Maier T, Follmann M, Hessler G, Kleemann HW, Hachtel S, Fuchs B, Weissmann N, Linz W, Schmidt T, Löhn M, Schroeter K, Wang L, Rütten H, Strübing C. Discovery and pharmacological characterization of a novel potent inhibitor of diacylglycerol-sensitive TRPC cation channels. Br J Pharmacol. 2015 Jul;172(14):3650-60. doi: 10.1111/bph.13151. Epub 2015 May 19. PMID: 25847402; PMCID: PMC4507166.
1: Maier T, Follmann M, Hessler G, Kleemann HW, Hachtel S, Fuchs B, Weissmann N, Linz W, Schmidt T, Löhn M, Schroeter K, Wang L, Rütten H, Strübing C. Discovery and pharmacological characterization of a novel potent inhibitor of diacylglycerol-sensitive TRPC cation channels. Br J Pharmacol. 2015 Jul;172(14):3650-60. doi: 10.1111/bph.13151. Epub 2015 May 19. PubMed PMID: 25847402; PubMed Central PMCID: PMC4507166. 2: Ilatovskaya DV, Palygin O, Levchenko V, Endres BT, Staruschenko A. The Role of Angiotensin II in Glomerular Volume Dynamics and Podocyte Calcium Handling. Sci Rep. 2017 Mar 22;7(1):299. doi: 10.1038/s41598-017-00406-2. PubMed PMID: 28331185; PubMed Central PMCID: PMC5428415. 3: 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.