TRP Channel Modulator

Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC₅₀: 60 nM, K_d: 40 nM), with blood-brain barrier permeability. Rosiglitazone is an TRPC5 activator (EC₅₀: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer.

Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC₅₀s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a K_d of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).

Rosiglitazone (BRL 49653) hydrochloride is an orally active selective PPARγ agonist (EC₅₀: 60 nM, K_d: 40 nM). Rosiglitazone hydrochloride is a TRPC5 activator (EC₅₀: 30 μM) and TRPM3 inhibitor. Rosiglitazone hydrochloride can be used in the research of obesity and diabetes, senescence, ovarian cancer.

Pulegone is a monoterpene ketone compound widely present in the essential oils of many plants. Pulegone can also be used as a bird repellent. Pulegone has multiple activities such as anti-inflammatory, antibacterial, antifungal, and anti-hyperalgesic effects. Pulegone is particularly effective against bacteria of the Salmonella species.

Rosiglitazone (Standard) is the analytical standard of Rosiglitazone. This product is intended for research and analytical applications. Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC₅₀: 60 nM, K_d: 40 nM). Rosiglitazone is an TRPC5 activator (EC₅₀: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer.

RN-1747 is a selective TRPV4 channel agonist, with EC₅₀ values of 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4, respectively. RN-1747 acts as an antagonist of TRPM8, with an IC₅₀ of 4 μM. Topical cutaneous administration of RN-1747 induces hypothermia, increases tail heat loss via cutaneous vasodilation, and promotes cold-seeking behavior in rats. Intracerebroventricular administration of RN-1747 does not induce hypothermia in rats.

Afidopyropen (ME-5343) is an Afidopyropen targets sucking insects such as whiteflies, aphids, and leafhoppers by acting on the Nanchung (Nan) and Inactive (Iav) encoding gene of insects, and affecting TRPV channel. Afidopyropen can be used for many crops for its degradability.

Rosiglitazone-d₄ is deuterated labeled Rosiglitazone (HY-17386). Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC₅₀: 60 nM, K_d: 40 nM). Rosiglitazone is an TRPC5 activator (EC₅₀: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer.

Rosiglitazone-d₃ is the deuterium labeled Rosiglitazone. Rosiglitazone (BRL 49653) is a selective, orally active PPARγ agonist with EC₅₀s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively. Rosiglitazone binds to PPARγ with a Kd of approximately 40 nM. Rosiglitazone is also an activator of TRPC5 (EC₅₀=~30 μM) and an inhibitor of TRPM3.

Rosiglitazone (BRL 49653) potassium is an orally active selective PPARγ agonist (EC₅₀: 60 nM, K_d: 40 nM). Rosiglitazone potassium is a TRPC5 activator (EC₅₀: 30 μM) and TRPM3 inhibitor. Rosiglitazone potassium can be used in the research of obesity and diabetes, senescence, ovarian cancer.

AMG-8562 is a TRPV1 modulator. AMG-8562 blocks Capsaicin (HY-10448) activation of TRPV1 without affecting heat activation of TRPV1. AMG-8562 potentiates pH 5 activation of TRPV1. AMG-8562 blocks capsaicin-induced flinching behavior in pain models. AMG-8562 produces significant efficacy in CFA- and skin incision-induced thermal hyperalgesia, and in the Acetic acid (HY-Y0319)-induced writhing models.

Rosiglitazone (maleate) (Standard) is the analytical standard of Rosiglitazone (maleate). This product is intended for research and analytical applications. Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC₅₀s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a K_d of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).

TRPC5 modulator-1 (Compound 9) is a TRPC5 modulator with an IC₅₀ of <1 nM for the research of neuropsychiatry disorders.

KJM429 (MK-056) is a high-affinity ligand for the rat vanilloid receptor rTRPV1 (K_i=30-63 nM) with a unique dual regulatory function. KJM429 acts as a competitive antagonist to inhibit TRPV1 receptor activation induced by Capsaicin (HY-10448), resiniferatoxin, thermal stimulation and weak acid (pH 6.0), and switches to a TRPV1 agonist under strong acid conditions (pH<5.5). KJM429 effectively blocks calcium influx induced by Capsaicin and partial thermal stimulation, and triggers calcium uptake under low pH conditions, with minimal effects on non-TRPV1-mediated calcium signaling. KJM429 can be used for research on the mechanisms of pain-related diseases such as postherpetic neuralgia, diabetic neuropathy, cluster headache, osteoarthritis and pruritus.

Cannabitwinol is a selective thermosensitive TRP modulator and NF-κB inhibitor. Cannabitwinol inhibits TNFα-induced NF-κB-driven transcription and TNFα-induced IL-8 release, and exhibits anti-inflammatory and antioxidant activities. Cannabitwinol shows selectivity for cold-activated TRP channels, activating TRPA1 (EC₅₀ = 3.0 μM) and antagonizing TRPM8 (IC₅₀ = 3.9 μM), but has no significant affinity for heat-activated TRP channels such as TRPV1 and TRPV2. Cannabitwinol can be used in research related to inflammatory skin diseases, cold allodynia, and hyperalgesia.

Rosiglitazone-d₄-1 (BRL 49653-d₄-1) is deuterium-labeled Rosiglitazone (HY-17386).

MRS 1477, a dihydropyridine derivative, is a positive allosteric modulator of TRPV1 in the presence of capsaicin. MRS 1477 itself does not induce apoptosis, but the co-existence of MRS 1477 and capsaicin can induce apoptosis.

PQM-244 (Compound 5c) is an orally active and multi-target modulator of TRPV1 and CB1 and CB2 receptors. PQM-244 has significant peripheral antinociceptive effects on both neurogenic and inflammatory phases. PQM-244 also has potential antioxidant activity with an IC₅₀  of  14.15 µM for radical scavenging DPPH. PQM-244 can be used for chronic pain and inflammatory disease research, such as diabetes, atherosclerosis and Alzheimer’s disease.

Palvanil is a Capsaicin (HY-10448) analogue, shows strong desensitizing capability against the TRPV1 receptor. Palvanil shows anti-nociceptive and anti-inflammation effects.

Pulegone-d₈ is deuterated labeled Pulegone (HY-N1500). Pulegone is a monoterpene ketone compound widely present in the essential oils of many plants. Pulegone can also be used as a bird repellent. Pulegone has multiple activities such as anti-inflammatory, antibacterial, antifungal, and anti-hyperalgesic effects. Pulegone is particularly effective against bacteria of the Salmonella species.