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TRP Channel Transient Receptor Potential Channels

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TRP Channel Transient Receptor Potential Channels TRP Channel Transient receptor potential channels TRP Channel (Transient receptor potential channel) is a group of ion channels located mostly on the plasma membrane of numerous human and animal cell types. 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 vanilloid), TRPM ("M" for melastatin), TRPN, and TRPA. In group 2, there are TRPP ("P" for polycystic) and TRPML ("ML" for mucolipin). Many of these channels mediate a variety of sensations like the sensations of pain, hotness, warmth or coldness, different kinds of tastes, pressure, and vision. TRP channels are relatively non-selectively permeable to cations, including sodium, calcium and magnesium. TRP channels are initially discovered in trp-mutant strain of the fruit fly Drosophila. Later, TRP channels are found in vertebrates where they are ubiquitously expressed in many cell types and tissues. TRP channels are important for human health as mutations in at least four TRP channels underlie disease. www.MedChemExpress.com 1 TRP Channel Antagonists, Inhibitors, Agonists, Activators & Modulators (-)-Menthol (E)-Cardamonin Cat. No.: HY-75161 ((E)-Cardamomin; (E)-Alpinetin chalcone) Cat. No.: HY-N1378 (-)-Menthol is a key component of peppermint oil (E)-Cardamonin ((E)-Cardamomin) is a novel that binds and activates transient receptor antagonist of hTRPA1 cation channel with an IC50 potential melastatin 8 (TRPM8), a of 454 nM. Ca2+-permeable nonselective cation channel, to 2+ increase [Ca ]i. Antitumor activity. Purity: ≥98.0% Purity: 99.81% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 500 mg, 1 g Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg (Z)-Capsaicin 1,4-Cineole (Zucapsaicin; Civamide; cis-Capsaicin) Cat. No.: HY-B1583 Cat. No.: HY-N7117 (Z)-Capsaicin is the cis isomer of capsaicin, acts 1,4-Cineole is a widely distributed, natural, as an orally active TRPV1 agonist, and is used in oxygenated monoterpene. 1,4-Cineole, present in the research of neuropathic pain. eucalyptus oil, activates both human TRPM8 and human TRPA1. Purity: 99.96% Purity: ≥95.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 50 mg Size: 10 mM × 1 mL, 100 mg 2-Aminoethyl diphenylborinate 8-Gingerol (2-APB) Cat. No.: HY-W009724 Cat. No.: HY-N0447 2-Aminoethyl diphenylborinate (2-APB) is a 8-Gingerol, found in the rhizomes of ginger (Z. cell-permeable inhibitor of IP3R. 2-Aminoethyl officinale) with oral bioavailability, activates diphenylborinate also inhibits the store-operated TRPV1, with an EC50 of 5.0 µM. 8-Gingerol Ca2+ (SOC) channel and activates some TRP inhibits COX-2, and inhibits the growth of H. pylori channels (V1, V2 and V3). in vitro. Purity: 98.03% Purity: 99.65% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 20 mg A-1165442 A-967079 Cat. No.: HY-12428 Cat. No.: HY-108463 A-1165442 is a potent, competitive and orally A-967079 is a selective TRPA1 receptor antagonist available TRPV1 antagonist with an IC50 of 9 nM with IC50s of 67 nM and 289 nM at human and rat for human TRPV1. TRPA1 receptors, respectively, and has good penetration into the CNS. Purity: 99.70% Purity: 98.83% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg ABT-239 AC1903 Cat. No.: HY-12195 Cat. No.: HY-122051 ABT-239 is a novel, highly efficacious, AC1903 is a specific and selective inhibitor of non-imidazole class of H3R antagonist and a TRPC5 and has podocyte-protective properties. transient receptor potential vanilloid type 1 AC1903 does no effects on TRPC4 or TRPC6 currents (TRPV1) antagonist. and shows no off-target effects in kinase profiling assays. Purity: 99.06% Purity: 98.64% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Adenosine 5′-diphosphoribose sodium AM-0902 (ADP ribose sodium) Cat. No.: HY-100973A Cat. No.: HY-108329 Adenosine 5′-diphosphoribose sodium (ADP ribose AM-0902 is a potent, selective transient receptor sodium) is a nicotinamide adenine nucleotide potential A1 (TRPA1) antagonist with IC50s of 71 (NAD+) metabolite. Adenosine 5′-diphosphoribose and 131 nM for rTRPA1 and hTRPA1, respectively. sodium is the most potent and primary intracellular Ca2+-permeable cation TRPM2 channel activator. Purity: ≥98.0% Purity: 99.67% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg AM12 AMG 333 Cat. No.: HY-128561 Cat. No.: HY-112703 AM12 inhibits Lanthanide-evoked TRPC5 activity AMG 333 is a potent and highly selective TRPM8 with an IC50 of 0.28 μM. antagonist with an IC50 of 13 nM. Purity: >98% Purity: 99.76% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg AMG 517 AMG2850 Cat. No.: HY-10634 Cat. No.: HY-104059 AMG 517 is a potent and selective vanilloid AMG2850 is a potent, orally bioavailable and receptor-1 (TRPV1) antagonist with an IC50 of 0.5 selective transient receptor potential melastatin 8 nM. (TRPM8) antagonist. Purity: 99.97% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 1 mg, 5 mg AMG9810 Amiloride Cat. No.: HY-101736 (MK-870) Cat. No.: HY-B0285 AMG9810 is a selective and competitive vanilloid Amiloride (MK-870) is an inhibitor of both receptor 1 (TRPV1) antagonist with IC50 values of epithelial sodium channel (ENaC) and 24.5 and 85.6 nM for human and rat TRPV1, urokinase-type plasminogen activator receptor repectively. (uTPA). Amiloride is a blocker of polycystin-2 (PC2; TRPP2) channel. Purity: 99.76% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg Amiloride hydrochloride Amiloride hydrochloride dihydrate (MK-870 hydrochloride) Cat. No.: HY-B0285A (MK-870 hydrochloride dihydrate) Cat. No.: HY-B0285B Amiloride hydrochloride (MK-870 hydrochloride) is Amiloride hydrochloride dihydrate (MK-870 an inhibitor of both epithelial sodium channel hydrochloride dihydrate) is an inhibitor of both (ENaC) and urokinase-type plasminogen activator epithelial sodium channel (ENaC) and receptor (uTPA). Amiloride hydrochloride is a urokinase-type plasminogen activator receptor blocker of polycystin-2 (PC2; TRPP2) channel. (uTPA). Amiloride hydrochloride dihydrate is a blocker of polycystin-2 (PC2; TRPP2) channel. Purity: 99.71% Purity: 99.50% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 100 mg, 500 mg Size: 10 mM × 1 mL, 100 mg www.MedChemExpress.com 3 AP-18 AS1269574 Cat. No.: HY-W014421 Cat. No.: HY-107535 AP-18, a potent and selective TRPA1 inhibitor, AS1269574 is a potent, orally available GPR119 blocks activation of TRPA1 by 50 μM Cinnamaldehyde agonist, with an EC50 of 2.5 μM in HEK293 cells with an IC50 of 3.1 μM and 4.5 μM for human and expressing human GPR119. AS1269574 activates TRPA1 mouse TRPA1, respectively. AP-18 reverses complete cation channels to stimulate glucagon-like Freund's adjuvant (CFA)-induced mechanical peptide-1 (GLP-1) secretion. hyperalgesia in mice. Purity: >98% Purity: 98.76% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Asivatrep ASP7663 (PAC-14028) Cat. No.: HY-12777 Cat. No.: HY-101907 Asivatrep (PAC-14028) is a potent and selective ASP7663 is an orally active and selective TRPA1 transient receptor potential vanilloid type I agonist. ASP7663 exerts both anti-constipation and (TRPV1) antagonist. anti-abdominal pain actions. Purity: 95.14% Purity: 99.16% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg BCTC Beta-Eudesmol Cat. No.: HY-19960 Cat. No.: HY-N6018 BCTC is a potent and specific inhibitor of Beta-Eudesmol is a natural oxygenated transient receptor potential cation channel sesquiterpene, activates hTRPA1, with an EC50 subfamily M member 8 (TRPM8) in prostate cancer of 32.5 μM. Beta-Eudesmol increases appetite (PCa) DU145 cells. through TRPA1. Purity: 97.23% Purity: 96.54% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 20 mg BI-749327 Bisandrographolide C Cat. No.: HY-111925 Cat. No.: HY-N2941 BI-749327 is a potent, high selectivity and orally Bisandrographolide C is an unusual dimer of bioavailable TRPC6 antagonist, with IC50s of 13 ent-labdane diterpenoid isolated and identified nM, 19 nM and 15 nM for mouse, human and guinea from Andrographis paniculata. pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7. Purity: 99.53% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg Caffeic acid Camphor Cat.
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