ZINC17988990

	ZINC17988990 ZINC17988990 is a drug which acts as a potent and selective inhibitor for the TRPV5 calcium channel, with an IC50 of 177 nM and high selectivity for TRPV5 over TRPV6 and the other subtypes of TRPV. It is the first selective inhibitor to be developed for TRPV5, and may be useful for modulating calcium reabsorption in the kidneys. See also * HC-067047 * SET2 SET2 is a drug which acts as a selective antagonist for the TRPV2 receptor. It is moderately potent with an IC50 of 460nM, but is highly selective for TRPV2 over the other subtypes of TRPV, and is the first such compound to be developed. A role ... References {{pharm-stub Experimental drugs ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]
	TRPV5 Transient receptor potential cation channel subfamily V member 5 is a calcium channel protein that in humans is encoded by the ''TRPV5'' gene. Function The ''TRPV5'' gene is a member of the transient receptor family and the TRPV subfamily. The calcium-selective channel, TRPV5, encoded by this gene has 6 transmembrane-spanning domains, multiple potential phosphorylation sites, an N-linked glycosylation site, and 5 ANK repeats. This protein forms homotetramers or heterotetramers and is activated by a low internal calcium level. Both TRPV5 and TRPV6 are expressed in kidney and intestinal epithelial cells. TRPV5 is mainly expressed in kidney epithelial cells, where it plays an important role in the reabsorption of Ca2+, whereas TRPV6 is mainly expressed in the intestine. The enzyme α-klotho increases kidney calcium reabsorption by stabilizing TPRV5. Klotho is a beta-glucuronidase-like enzyme that activates TRPV5 by removal of sialic acid. Clinical significance Normal ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]
	HC-067047 HC-067047 is a drug which acts as a potent and selective antagonist for the TRPV4 Transient receptor potential cation channel subfamily V member 4 is an ion channel protein that in humans is encoded by the ''TRPV4'' gene. The ''TRPV4'' gene encodes TRPV4, initially named "vanilloid-receptor related osmotically activated channe ... receptor. It has been used to investigate the role of TRPV4 receptors in a number of areas, such as regulation of blood pressure, bladder function and some forms of pain, as well as neurological functions. See also * JWH-147 * RN-9893 * SET2 * ZINC17988990 References Pyrroles {{pharm-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]
	SET2 SET2 is a drug which acts as a selective antagonist for the TRPV2 receptor. It is moderately potent with an IC50 of 460nM, but is highly selective for TRPV2 over the other subtypes of TRPV, and is the first such compound to be developed. A role has been suggested for TRPV2 in tumor metastasis, making this a target of interest in the treatment of cancer. See also * HC-067047 HC-067047 is a drug which acts as a potent and selective antagonist for the TRPV4 Transient receptor potential cation channel subfamily V member 4 is an ion channel protein that in humans is encoded by the ''TRPV4'' gene. The ''TRPV4'' gene en ... * ZINC17988990 References Thioethers Pyrimidines {{pharm-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]
picture info	TRPV6 TRPV6 is a membrane calcium (Ca2+) channel protein which is particularly involved in the first step in Ca2+absorption in the intestine. Classification Transient Receptor Potential Vanilloid subfamily member 6 (TRPV6) is an epithelial Ca2+ channel that belongs to the transient receptor potential family (TRP) of proteins. The TRP family is a group of channel proteins critical for ionic homeostasis and the perception of various physical and chemical stimuli. TRP channels can detect temperature, osmotic pressure, olfaction, taste, and mechanical forces. The human genome encodes for 28 TRP channels, which include six TRPV channels. The high Ca2+-selectivity of TRPV5 and TRPV6 makes these channels distinct from the other four TRPV channels (TRPV1-TRPV4). TRPV5 and TRPV6 are involved in Ca2+ transport, whereas TRPV1 through TRPV3 are heat sensors with different temperature threshold for activation, and TRPV4 is involved in sensing osmolarity. Genetic defects in TRPV6 gene are lin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]
	TRPV TRPV is a family of transient receptor potential cation channels (TRP channels) in animals. All TRPVs are highly calcium selective. TRP channels are a large group of ion channels consisting of six protein families, located mostly on the plasma membrane of numerous human and animal cell types, and in some fungi. TRP channels were initially discovered in the ''trp'' mutant strain of the fruit fly ''Drosophila'' that displayed transient elevation of potential in response to light stimuli, and were therefore named "transient receptor potential" channels. The name now refers only to a family of proteins with similar structure and function, not to the mechanism of their activation. Later, TRP channels were found in vertebrates where they are ubiquitously expressed in many cell types and tissues. There are about 28 TRP channels that share some structural similarity to each other. These are grouped into two broad groups: group 1 includes TRPC ( "C" for canonical), TRPV ("V" for vani ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]