| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
CaCCinh-A01 (also known as TMEM16 Blocker I) is an inhibitor of TMEM16A and calcium-activated chloride channel (CaCC) with IC50s of 2.1 and 10 μM, respectively. TMEM16A (ANO1) functions as a calcium-activated chloride channel (CaCC). CaCCs are widely expressed in mammalian tissues, including intestinal epithelia, where they facilitate fluid secretion. CaCCinh-A01 is a non-selective inhibitor of CaCCs that blocks ATP-stimulated chloride conductance in human salivary gland, intestinal, and bronchial epithelium (mean IC50 = 10 µM). As a TMEM16A/CaCC inhibitor, CaCCinh-A01 is a potential development candidate for drug therapy of hypertension, pain, diarrhea, and excessive mucus production.
| ln Vitro |
After ATP stimulation, CaCC current is strongly inhibited by 30 μM CaCCinh-A01 and 100 μM tannic acid[1]. 0.1, 1 and 10 μM CaCCinh-A01 reduces calcium-dependent chloride current by 38±14, 66±10 and 91±1%, respectively. When ATP-induced short-circuit currents are present at 10 and 30 μM CaCCinh-A01, respectively, they are decreased by 38±7 and 78±3%[2].
|
|---|---|
| ln Vivo |
In a middle cerebral artery occlusion model in mice, CaCCinh-A01 (vein injection; 5 mg/kg; caudal vein injection within 15 min after the onset of reperfusion) significantly reduces infarction when compared with MCAO-saline treatment at 24 h or 72 h[3].
|
| Animal Protocol |
Animal/Disease Models: Two-month-old male C57/BL6J mice[3]
Doses: 5 mg/kg Route of Administration: Vein injection; 5 mg/kg; caudal vein injection within 15 min after the onset of reperfusion Experimental Results: Attenuated brain infarct size, improved neurological outcomes and lowered BBB permeability after ischemic stroke in mice. |
| References |
[1]. TMEM16A inhibitors reveal TMEM16A as a minor component of calcium-activated chloridechannel conductance in airway and intestinal epithelial cells. J Biol Chem. 2011 Jan 21;286(3):2365-74.
[2]. De La Fuente R, et al. Small-molecule screen identifies inhibitors of a human intestinal calcium-activated chloridechannel. Mol Pharmacol. 2008 Mar;73(3):758-68. [3]. Pin-Yi Liu, et al. TMEM16A Inhibition Preserves Blood-Brain Barrier Integrity After Ischemic Stroke.Front Cell Neurosci. 2019 Aug 6;13:360. |
| Molecular Formula |
C18H21NO4S
|
|
|---|---|---|
| Molecular Weight |
347.43
|
|
| CAS # |
407587-33-1
|
|
| Related CAS # |
|
|
| SMILES |
O=C(C1=C(NC(C2=CC=CO2)=O)SC3=C1CCC(C(C)(C)C)C3)O
|
|
| Synonyms |
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.20 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.20 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.20 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8783 mL | 14.3914 mL | 28.7828 mL | |
| 5 mM | 0.5757 mL | 2.8783 mL | 5.7566 mL | |
| 10 mM | 0.2878 mL | 1.4391 mL | 2.8783 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 Chemical structures of TMEM16A inhibitors.J Biol Chem.2011 Jan 21;286(3):2365-74. |
|---|
 TMEM16A inhibitors block the initial transient CaCC current in human intestinal epithelial cells following agonist stimulation.J Biol Chem.2011 Jan 21;286(3):2365-74. |
 TMEM16A inhibitors poorly block CaCC chloride current in human bronchial epithelial cells.J Biol Chem.2011 Jan 21;286(3):2365-74. |
 Identification of small molecule inhibitors of human TMEM16A.J Biol Chem.2011 Jan 21;286(3):2365-74. |
|---|
 TMEM16A inhibitors block CaCC chloride current in human salivary gland epithelial cells.J Biol Chem.2011 Jan 21;286(3):2365-74. |
 IL-4 induced CaCC up-regulation in CF human bronchial epithelial cells.J Biol Chem.2011 Jan 21;286(3):2365-74. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA