TMEM16AInhibitorsRevealTMEM16A(T16Ainh-A01) Property

Melting point:

211-212°C (dec.)

Density 

1.39±0.1 g/cm3(Predicted)

storage temp. 

room temp

solubility 

DMSO: soluble5mg/mL, clear (warmed)

pka

7.20±0.50(Predicted)

form 

powder

color 

white to beige

Safety

Hazard Codes 

Xi

Risk Statements 

36/37/38

Safety Statements 

26

WGK Germany 

3

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

TMEM16AInhibitorsRevealTMEM16A(T16Ainh-A01) Chemical Properties,Usage,Production

Uses

This compound functions as a selective class A inhibitor of the calcium activated chloride channel TMEM16A. Useful in the treatment of hypertension, pain, diarrhea and mucus overproduction.

Uses

T16Ainh-A01 has been used as an inhibitor of transmembrane protein 16A (TMEM16A).

Uses

TMEM16AInhibitorsRevealTMEM16A(T16Ainh-A01) compound functions as a selective class A inhibitor of the calcium activated chloride channel TMEM16A. Useful in the treatment of hypertension, pain, diarrhea and mucus overproduction.

General Description

An aminophenylthiazole that acts as an inhibitor of TMEM16A channel, a calcium-activated chloride channel (CaCC) (IC₅₀ = 1.1 μM). Fully blocks CaCC current in salivary gland cells at 10 μM, but has very little effect in airway and intestinal cells, which is consistent with the observation of RNAi knock-down. Completely blocks chloride currents produced by TMEM16A Activator, Eact (Cat. No. 631547) at 10 μM. In addition, shown to block calcium-activated chloride channels in vascular smooth muscle cells, and relaxes murine and human blood vessels.

Biochem/physiol Actions

T16Ainh-A01 is a selective TMEM16A calcium-activated chloride channel inhibitor that strongly inhibits chloride current in salivary gland cells. T16Ainh-A01 poorly inhibited total CaCC current in intestinal and airway epithelial cells, but blocked mainly an initial, agonist-stimulated transient chloride current. T16Ainh-A01 does not alter cytoplasmic calcium and has little effect on CFTR Cl- conductance.

storage

Store at +4°C