desensitizing

By Targets:	Calcium Channel (1) Cannabinoid Receptor (1) Cytochrome P450 (1) Endogenous Metabolite (1) GABA Receptor (1) iGluR (4) mAChR (2) nAChR (3) NO Synthase (2) PKA (1) PKC (1) ROCK (1) Sodium Channel (1) TRP Channel (1)
By Research Areas:	Cardiovascular Disease (1) Inflammation/Immunology (2) Metabolic Disease (1) Neurological Disease (13)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-121027

Anagyrine (-)-Anagyrine; Monolupine; Rhombinine	mAChR nAChR	Neurological Disease
Anagyrine ((-)-Anagyrine) is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine binds to muscarinic and nicotinic acetylcholine receptors with IC₅₀ values of 132 and 2096 µM respectively. Anagyrine is a potent and effective desensitizer of nAChR, and Anagyrine can directly, without metabolism, desensitize nAChR .

HY-121027A

Anagyrine hydrochloride (-)-Anagyrine hydrochloride; Monolupine hydrochloride; Rhombinine hydrochloride	mAChR nAChR	Neurological Disease
Anagyrine ((-)-Anagyrine) hydrochloride is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine hydrochloride binds to muscarinic and nicotinic acetylcholine receptors with IC₅₀ values of 132 and 2096 µM respectively. Anagyrine hydrochloride is a potent and effective desensitizer of nAChR, and Anagyrine hydrochloride can directly, without metabolism, desensitize nAChR .

HY-124906

JAMI1001A	iGluR	Neurological Disease
JAMI1001A is a positive allosteric modulator of AMPA receptor. JAMI1001A efficaciously modulates AMPA receptor deactivation and desensitization of both flip and flop receptor isoforms .

HY-103229

Cl-HIBO	iGluR	Neurological Disease
Cl-HIBO is a highly subtype-selective GluR1/2 agonist (EC₅₀=4.7 and 1.7 μM, respectively). Cl-HIBO is a potent AMPA receptor agonist (IC₅₀=0.22 μM). Cl-HIBO has desensitizing properties .

HY-P3785

PKI(5-22)amide	PKA	Neurological Disease
PKI(5-22)amide is the active inhibitory fragment of the inhibitor of the cyclic AMP-dependent protein kinase (PKA). PKI(5-22)amide inhibits PKA activation, but fails to attenuate homologous desensitization of CRF1 receptors .

HY-101165

Cyclothiazide
Cyclothiazide, a positive allosteric modulator of AMPA receptors, is used frequently to block the desensitization of both native and heterologously expressed AMPA receptors. Cyclothiazide is known to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current .

HY-137988

Palvanil	TRP Channel	Neurological Disease Inflammation/Immunology
Palvanil is a Capsaicin (HY-10448) analogue, shows strong desensitizing capability against the TRPV1 receptor. Palvanil shows anti-nociceptive and anti-inflammation effects .

HY-P5876

Proadrenomedullin (N-20) (bovine, porcine) ProADM N20(bovine, porcine); PAMP-20(bovine, porcine)	nAChR	Neurological Disease
Proadrenomedullin (N-20) (ProADM N20) (bovine, porcine) is a potent and noncompetitive hypotensive and catecholamine release-inhibitory peptide released from chromaffin cells. Proadrenomedullin (N-20) (bovine, porcine) inhibits catecholamine secretion with an IC₅₀ of 350 nM in PC12 pheochromocytoma cells. Proadrenomedullin (N-20) (bovine, porcine) also blocks (EC₅₀≈270 nM) nicotinic cholinergic agonist desensitization of catecholamine release, as well as desensitization of nicotinic signal transduction ( ²²Na ⁺ uptake) .

HY-N4323

14-Deoxyandrographolide	Calcium Channel	Neurological Disease Metabolic Disease
14-Deoxyandrographolide is a labdane diterpene with calcium channel blocking activity. 14-Deoxyandrographolide desensitizes hepatocytes to TNF-α-mediated apoptosis through the release of TNFRSF1A release .

HY-119943B

(R)-PF-06256142	Others	Neurological Disease
(R)-PF-06256142 is the R enantiomer of PF-06256142 with low active. PF-06256142 is a potent and selective orthosteric D1 receptor agonist that can reduce receptor desensitization relative to dopamine and other catechol-containing agonists .

HY-B0822S1

Fipronil-13C6	GABA Receptor Cytochrome P450	Inflammation/Immunology
Fipronil- ¹³C₆ is the ¹³C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.

HY-103045

CMPD101 3 Publications Verification	PKC ROCK	Cardiovascular Disease
CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC₅₀ of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC₅₀s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure .

HY-161118

MB327	Others	Neurological Disease
MB327 is a bipyridine nonoxime compound that restores neuromuscular function. MB327 restores the activity of nicotinamide acetylcholine receptors (nAChRs) for carbachol desensitization in a typical type II PAM manner. MB327 can neutralize nerve agent poisoning .

HY-W001160

5-Hydroxyindole	Endogenous Metabolite	Others
5-Hydroxyindole, a hydroxylated indole, can be found in a vast array of pharmacologically active agents and natural products. 5-Hydroxyindole slows desensitization of the 5-HT3 receptor-mediated ion current in N1E-115 neuroblastoma cells .

HY-100939

4-Chlorophenylguanidine hydrochloride	Sodium Channel	Neurological Disease
4-Chlorophenylguanidine hydrochloride is a potent ASIC3 positive allosteric modulator and reverses the effects of ASIC3 desensitization. 4-Chlorophenylguanidine hydrochloride influences ASIC3 activity through directly activating the channel and increasing proton sensitivity. 4-Chlorophenylguanidine hydrochloride offers a chemical backbone for the design of new ASIC3 ligands to study ASIC3 in vivo .

HY-P2307A

Tat-NR2Baa TFA	iGluR NO Synthase	Neurological Disease
Tat-NR2BAA TFA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA TFA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95 .

HY-P2307

Tat-NR2Baa	iGluR NO Synthase	Neurological Disease
Tat-NR2BAA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95 .

HY-150057

CB1R Allosteric modulator 4	Cannabinoid Receptor	Others
CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment .

Cat. No.	Product Name	Target	Research Area

HY-P2307

Tat-NR2Baa	iGluR NO Synthase	Neurological Disease
Tat-NR2BAA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95 .

HY-P3785

PKI(5-22)amide	PKA	Neurological Disease
PKI(5-22)amide is the active inhibitory fragment of the inhibitor of the cyclic AMP-dependent protein kinase (PKA). PKI(5-22)amide inhibits PKA activation, but fails to attenuate homologous desensitization of CRF1 receptors .

HY-P5876

Proadrenomedullin (N-20) (bovine, porcine) ProADM N20(bovine, porcine); PAMP-20(bovine, porcine)	nAChR	Neurological Disease
Proadrenomedullin (N-20) (ProADM N20) (bovine, porcine) is a potent and noncompetitive hypotensive and catecholamine release-inhibitory peptide released from chromaffin cells. Proadrenomedullin (N-20) (bovine, porcine) inhibits catecholamine secretion with an IC₅₀ of 350 nM in PC12 pheochromocytoma cells. Proadrenomedullin (N-20) (bovine, porcine) also blocks (EC₅₀≈270 nM) nicotinic cholinergic agonist desensitization of catecholamine release, as well as desensitization of nicotinic signal transduction ( ²²Na ⁺ uptake) .

HY-P2307A

Tat-NR2Baa TFA	iGluR NO Synthase	Neurological Disease
Tat-NR2BAA TFA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA TFA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-121027

Anagyrine (-)-Anagyrine; Monolupine; Rhombinine	Alkaloids Piperidine Alkaloids Structural Classification Classification of Application Fields Leguminosae Source classification Plants Disease Research Fields Lupinus albus Linn. Cancer	mAChR nAChR
Anagyrine ((-)-Anagyrine) is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine binds to muscarinic and nicotinic acetylcholine receptors with IC₅₀ values of 132 and 2096 µM respectively. Anagyrine is a potent and effective desensitizer of nAChR, and Anagyrine can directly, without metabolism, desensitize nAChR .

HY-N4323

14-Deoxyandrographolide	Andrographis paniculata (Burm. F.) Nees Acanthaceae Terpenoids Source classification Diterpenoids Plants	Calcium Channel
14-Deoxyandrographolide is a labdane diterpene with calcium channel blocking activity. 14-Deoxyandrographolide desensitizes hepatocytes to TNF-α-mediated apoptosis through the release of TNFRSF1A release .

HY-W001160

5-Hydroxyindole	Alkaloids Monophenols Classification of Application Fields Source classification Other Diseases Phenols Endogenous metabolite Disease Research Fields Indole Alkaloids	Endogenous Metabolite
5-Hydroxyindole, a hydroxylated indole, can be found in a vast array of pharmacologically active agents and natural products. 5-Hydroxyindole slows desensitization of the 5-HT3 receptor-mediated ion current in N1E-115 neuroblastoma cells .

HY-121027A

Anagyrine hydrochloride (-)-Anagyrine hydrochloride; Monolupine hydrochloride; Rhombinine hydrochloride	Structural Classification Alkaloids Piperidine Alkaloids Leguminosae Source classification Plants Sophora flavescens Aiton	mAChR nAChR
Anagyrine ((-)-Anagyrine) hydrochloride is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine hydrochloride binds to muscarinic and nicotinic acetylcholine receptors with IC₅₀ values of 132 and 2096 µM respectively. Anagyrine hydrochloride is a potent and effective desensitizer of nAChR, and Anagyrine hydrochloride can directly, without metabolism, desensitize nAChR .

HY-137988

Palvanil	Monophenols Capsicum annuum L. Source classification Solanaceae Plants	TRP Channel
Palvanil is a Capsaicin (HY-10448) analogue, shows strong desensitizing capability against the TRPV1 receptor. Palvanil shows anti-nociceptive and anti-inflammation effects .

Cat. No.	Product Name	Chemical Structure

HY-B0822S1

Fipronil-13C6
Fipronil- ¹³C₆ is the ¹³C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.

Fipronil-13C6

Fipronil- ¹³C₆ is the ¹³C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.

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