1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. TRP Channel
  3. Pyr10

Pyr10 

Cat. No.: HY-19408 Purity: 99.60%
Handling Instructions

Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels.

For research use only. We do not sell to patients.

Pyr10 Chemical Structure

Pyr10 Chemical Structure

CAS No. : 1315323-00-2

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10 mM * 1 mL in DMSO USD 73 In-stock
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50 mg USD 432 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels[1].

IC50 & Target[1]

TRPC3

0.72 μM (IC50)

In Vitro

Pyr10 has the ability to discriminate between the classical Orai-mediated, highly Ca2+ selective signalling pathway and the phospholipase C-dependent Ca2+ entry-mediated by TRPC channels, specifically by TRPC3. Pyr10 (3 μM) completely eliminates TRPC3 currents as well as Ca2+ entry while exerting modest effects on Orai-mediated responses. The selective block of TRPC3 channels by Pyr10 barely affected mast cell activation[1].

In Vivo

Genetic deletion (TRPC3-/-) and pharmacological channel blockade with Pyr10 blunts ventricular cardiac fibroblast activation and myocardial fibrosis in N(ω)-nitro-l-arginine methyl ester (l-NAME) hypertensive mice[2].

Molecular Weight

449.37

Formula

C₁₈H₁₃F₆N₃O₂S

CAS No.

1315323-00-2

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (222.53 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2253 mL 11.1267 mL 22.2534 mL
5 mM 0.4451 mL 2.2253 mL 4.4507 mL
10 mM 0.2225 mL 1.1127 mL 2.2253 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.56 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.56 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

Pyr10Pyr 10Pyr-10TRP ChannelTransient receptor potential channelsTRPC3OraipyrazoleROCESOCESTIM1Ca2+l-NAMEcardiacfibroblastInhibitorinhibitorinhibit

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Pyr10
Cat. No.:
HY-19408
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