1. Membrane Transporter/Ion Channel
  2. CRAC Channel

CM-4620 

Cat. No.: HY-101942 Purity: 99.94%
Handling Instructions

CM-4620 is a calcium-release activated calcium-channel (CRAC) inhibitor, with IC50s of 119, 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively.

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

CM-4620 Chemical Structure

CM-4620 Chemical Structure

CAS No. : 1713240-67-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 429 In-stock
Estimated Time of Arrival: December 31
5 mg USD 390 In-stock
Estimated Time of Arrival: December 31
10 mg USD 590 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1900 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2900 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

CM-4620 is a calcium-release activated calcium-channel (CRAC) inhibitor, with IC50s of 119, 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively.

IC50 & Target

IC50: 119 nM (Orai 1/STIM1), 895 nM (Orai 1/STIM1)[1].

In Vitro

It is determined that CM-4620 (compound 1) inhibits Orai 1/STIM1 channels with an IC50 of 119 nM, and Orai2/STIM1 channels with an IC50 of 895 nM. It is more potent on Orai1 than Orai2-type CRAC channels. In human PBMCs, CM-4620 potently inhibits release of multiple cytokines which play important roles in T cells (IC50s, IFN γ: 138 nM, IL-4: 879 nM, IL-6: 135 nM, IL-1β: 240 nM, IL-10: 303 nM, TNFα: 225 nM, IL-2: 59 nM, IL-17 120 nM)[1].

In Vivo

Mouse PACs are treated with CRAC inhibitors CM-4620 or GSK-7975A and monitored for their rate of Calcium uptake. Both CRAC inhibitors reduce the rate of store-operated Calcium entry into the ER to 50% of controllevels upon treatment with 700 nM of inhibitor. CM-4620 blocks 100% of reuptake at 10 mM[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (237.10 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3710 mL 11.8551 mL 23.7102 mL
5 mM 0.4742 mL 2.3710 mL 4.7420 mL
10 mM 0.2371 mL 1.1855 mL 2.3710 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.08 mg/mL (4.93 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (4.93 mM); Suspended solution; Need ultrasonic and warming

  • 3.

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

    Solubility: 2.08 mg/mL (4.93 mM); Suspended solution; Need ultrasonic and warming

References
Molecular Weight

421.76

Formula

C₁₉H₁₁ClF₃N₃O₃

CAS No.

1713240-67-5

SMILES

O=C(NC1=NC=C(C2=C(Cl)C=C(OC(F)(F)O3)C3=C2)N=C1)C4=C(C)C=CC=C4F

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.94%

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Product Name:
CM-4620
Cat. No.:
HY-101942
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CM-4620

Cat. No.: HY-101942