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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
22 Results for "
TRPV4 antagonist
" in MedChemExpress (MCE) Product Catalog:
Products (22)
22 Results for "TRPV4 antagonist" in MCE Product Catalog:
42
42 Publications Verification
Target:
Áreas de investigación:
HC-067047 is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 48 nM, 133 nM, and 17 nM, respectively .
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19 Cited Publications
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Áreas de investigación:
GSK2193874 is an orally active, potent, and selective TRPV4 antagonist with IC50s of 2 nM and 40 nM for rTRPV4 and hTRPV4 .
13
13 Cited Publications
Target:
Áreas de investigación:
GSK205 is a potent, selective TRPV4 antagonist with an IC50 of 4.19 μM for inhibiting TRPV4-mediated Ca 2+ influx .
10
10 Cited Publications
Referencia número: HY-19975
No. CAS: 946387-07-1
Target:
Áreas de investigación:
RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC50s for all three species (hTRPV4: 2.3 μM, mTRPV4: 5.9 μM, rTRPV4: 3.2 μM) . RN-1734 clearly decreases the production of tumor necrosis factor α (TNF-α) and interleukin 1β (IL-1β) without altering the number of olig2-positive cells .
9
9 Cited Publications
Referencia número: HY-18662
No. CAS: 1254205-52-1
Target:
Áreas de investigación:
RQ-00203078 is a highly selective, potent and orally active TRPM8 antagonist with IC50s of 5.3 nM and 8.3 nM for rat and human TRPM8 channels, respectively. RQ-00203078 shows little inhibitory action against TRPV1, TRPA1, TRPV4, or TRPM2 channels .
6
6 Cited Publications
Referencia número: HY-19976
No. CAS: 1024448-59-6
Target:
Áreas de investigación:
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 .
1
1 Cited Publications
Referencia número: HY-160900
No. CAS: 1803003-65-7
Target:
Áreas de investigación:
RN-1665 is an orally active TRPV4 antagonist that exhibits excellent selectivity for related TRP receptors such as TRPV1, TRPV3 and TRPM8. RN-1665 is a TRPV4 probe for focus screens, with IC50s of 0.26 μM and 0.39 μM for hTRPV4 and rTRPV4 from human and rat, respectively .
1
1 Cited Publications
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Áreas de investigación:
AMG2850 is an orally active, blood-brain barrier-permeable selective TRPM8 competitive antagonist. AMG2850 abolishes the counterirritant effect of TRPM8 agonists, blocks TRPM8 activation induced by cold, (-)-Menthol (HY-75161) and Icilin (HY-11062), and exhibits selectivity over TRPA1, TRPV1, TRPV3 and TRPV4. AMG2850 is applicable for pain-related research .
Referencia número: HY-160603
No. CAS: 1669444-50-1
Target:
Áreas de investigación:
PF-05214030 is a TRPV4 antagonist (IC50: 4 and 27nM for hTRPV4 and rTRPV4 respectively). PF-05214030 reverses the reduction in bladder capacity caused by intravesical infusion of a TRPV4 agonist .
Referencia número: HY-149823
No. CAS: 2918803-89-9
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Áreas de investigación:
TRPV4 antagonist 4 is a potent TRPV4 antagonist with an IC50 value of 22.65 nM. TRPV4 antagonist 4 inhibits TRPV4 current. TRPV4 antagonist 4 shows protective effects on acute lung injury .
Referencia número: HY-142620
No. CAS: 2681273-35-6
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Áreas de investigación:
TRPV4 antagonist 3 is a TRPV4 antagonist (pIC50 = 8.4).
Referencia número: HY-185006
No. CAS: 3026084-12-5
Target:
Áreas de investigación:
TRPV4 antagonist 5 (Example 21) is a TRPV4 antagonist .
Referencia número: HY-187364
No. CAS: 3050594-88-9
Target:
Áreas de investigación:
TRPV4 antagonist-7 is a potent and selective TRPV4 antagonist with an IC50 of 0.2 nM against human targets. TRPV4 antagonist-7 binds to the voltage-sensor-like domain cavity of TRPV4 and inhibits channel activity through the formation of salt bridges, hydrogen bonds, and edge-to-face π-stacking interactions. TRPV4 antagonist-7 induces phospholipid accumulation in HepG2 C3A cells in vitro with an IC50 of 3.8 μM, and exhibits moderate inhibitory effects on CYP2D6 with an IC50 of 5.1 μM. TRPV4 antagonist-7 dose-dependently inhibits GSK1016790A (HY-19608)-induced bronchoconstriction in rats and cough in guinea pigs. TRPV4 antagonist-7 can be used in studies related to respiratory system diseases .
Referencia número: HY-112202
No. CAS: 2215852-91-6
Target:
Áreas de investigación:
GSK3395879 is a selective and orally bioavailable transient receptor potential vanilloid-4 (TRPV4) antagonist with an IC50 of 1 nM for hTRPV4 .
Target:
Áreas de investigación:
RN-9893 is a potent and selective TRPV4 receptor antagonist with IC50 values of 320, 420 and 660 nM for mouse, human and rat channels, respectively .
Referencia número: HY-W721480
No. CAS: 1481646-76-7
Target:
Áreas de investigación:
HC-067047 hydrochloride is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 48 nM, 133 nM, and 17 nM, respectively .
Referencia número: HY-117372
No. CAS: 1445753-16-1
Target:
Áreas de investigación:
DFL23448 is a selective transient receptor potential melastatin-8 (TRPM8) antagonist. DFL23448 shows IC50 values of 10 and 21 nM in hTRPM8 human embryonic kidney 293 cells activated by Cooling Agent 10 or cold. DFL23448 has limited activity (IC50 >10 μM) at transient receptor potential vanilloids TRPV1, TRPA1, or TRPV4 or at various G protein-coupled receptors. DFL23448 can modify bladder function and reduce bladder overactivity in awake rats .
Referencia número: HY-110270A
No. CAS: 2109450-40-8
Target:
Áreas de investigación:
RN-9893 Hydrochloride is an orally active antagonist of transient receptor potential vanilloid 4 (TRPV4), with IC50 values of 0.42 and 0.66 μM, for humans and rats, respectively .
Referencia número: HY-100208R
No. CAS: 883031-03-6
Target:
Áreas de investigación:
HC-067047 (Standard) is the analytical standard of HC-067047 (HY-100208). This product is intended for research and analytical applications. HC-067047 is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 48 nM, 133 nM, and 17 nM, respectively .
Referencia número: HY-183906
No. CAS: 2215853-96-4
Target:
Áreas de investigación:
GSK3491943 is an antagonist of the transient receptor potential vanilloid subtype 4 (TRPV4) ion channel. GSK3491943 is applicable to research related to pulmonary edema induced by heart failure .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
