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Results for "

overactive

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adrenergic Receptor (7) Apoptosis (4) Autophagy (4) Calcium Channel (4) FAAH (1) Imidazoline Receptor (4) Isotope-Labeled Compounds (3) mAChR (18) Neurokinin Receptor (2) Phosphodiesterase (PDE) (2) Potassium Channel (4) PPAR (1) Prostaglandin Receptor (1) ROR (1)
By Research Areas:	Cancer (5) Cardiovascular Disease (5) Endocrinology (6) Inflammation/Immunology (1) Metabolic Disease (6) Neurological Disease (21)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-116408A

Propiverine hydrochloride	mAChR Calcium Channel	Neurological Disease
Propiverine hydrochloride is a bladder spasmolytic with calcium antagonistic and anticholinergic properties. Propiverine hydrochloride can be used for the research of overactive blaqdder and urinary incontinence .

HY-76570

(Rac)-5-Hydroxymethyl Tolterodine (Rac)-Desfesoterodine; (Rac)-PNU-200577	mAChR	Neurological Disease
(Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (K_i values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research .

HY-76570A

(Rac)-5-Hydroxymethyl Tolterodine hydrochloride (Rac)-Desfesoterodine hydrochloride; (Rac)-PNU-200577 hydrochloride	mAChR	Neurological Disease
(Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine) hydrochloride, an active metabolite of Tolterodine, is a mAChR antagonist (K_i values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine hydrochloride can be used for overactive bladder research .

HY-116408

Propiverine	mAChR	Neurological Disease
Propiverine is a potent antimuscarinic agent. Propiverine inhibits cellular calcium influx, thereby diminishing muscle spasm. Propiverine has neurotropic and musculotropic effects on the urinary bladder smooth muscle. Propiverine can used for overactive bladder (OAB) research .

HY-120961

Oleoyl ethyl amide N-Ethyloleamide	FAAH	Metabolic Disease
Oleoyl ethyl amide (N-Ethyloleamide) is a fatty acid amide hydrolase (FAAH) inhibitor. Oleoyl ethyl amide can counteract bladder overactivity .

HY-19933

Vibegron MK-4618	Adrenergic Receptor	Others
Vibegron (MK-4618) is a potent, highly selective and orally active β₃-adrenoceptor agonist (EC₅₀=1.1 nM). Vibegron can be used for severe urgency urinary incontinence related to overactive bladder .

HY-147226

EP3 antagonist 3	Prostaglandin Receptor	Neurological Disease Endocrinology
EP3 antagonist 3 (compound 2) is an orally active, potent and selective EP3 antagonist, with a pK_i of 8.3. EP3 antagonist 3 shows excellent pharmacokinetic properties. EP3 antagonist 3 can be used for overactive bladder (OAB) research .

HY-B0549A

Flavoxate hydrochloride Rec-7-0040; DW61	Phosphodiesterase (PDE) Calcium Channel mAChR	Neurological Disease
Flavoxate hydrochloride is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate hydrochloride is an antispasmodic agent and muscarinic mAChR antagonist. Flavoxate hydrochloride shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate hydrochloride can be used for the research of overactive bladder (OAB) and lower urinary tract infections .

HY-B0549

Flavoxate Rec-7-0040 free base; DW61 free base	Phosphodiesterase (PDE) Calcium Channel mAChR	Neurological Disease
Flavoxate is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate is an antispasmodic agent and muscarinic mAChR antagonist. Flavoxate shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate can be used for the research of overactive bladder (OAB) and lower urinary tract infections .

HY-148252

ADRA1D receptor antagonist 1 free base	Adrenergic Receptor	Endocrinology
ADRA1D receptor antagonist 1 (free base) (compound (R)-9s) is an orally active, potent and selective human α_1D-adrenoceptor (α_1D-AR) antagonist (K_i=1.6 nM). ADRA1D receptor antagonist 1 (free base) dose-dependently inhibits bladder contraction with an IC₃₀ value of 15 nM. ADRA1D receptor antagonist 1 (free base) can be used in studies of overactive bladder disorders such as urinary urgency, frequency and incontinence.

HY-A0030

Fesoterodine fumarate	mAChR	Neurological Disease Metabolic Disease
Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK_i values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .

HY-70053

Fesoterodine	mAChR	Neurological Disease Metabolic Disease
Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK_i values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB) .

HY-70053A

Fesoterodine L-mandelate	mAChR	Neurological Disease Metabolic Disease
Fesoterodine L-mandelate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK_i values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine L-mandelate is used for the overactive bladder (OAB) .

HY-160188

BAY-9683	PPAR	Cancer
BAY-9683 is an orally active covalent PPARG inverse agonist. BAY-9683 can be used in the study of diseases with overactive PPARG, such as luminal bladder cancer .

HY-116408AS

Propiverine-d7 hydrochloride	Isotope-Labeled Compounds mAChR Calcium Channel	Neurological Disease
Propiverine-d₇ (hydrochloride) is the deuterium labeled Propiverine hydrochloride. Propiverine hydrochloride is a bladder spasmolytic with calcium antagonistic and anticholinergic properties. Propiverine hydrochloride can be used for the research of overactive blaqdder and urinary incontinence[1][2].

HY-106659

SCH 900978 NK-1 Antagonist 1	Neurokinin Receptor	Neurological Disease Endocrinology
SCH 900978 (NK-1 Antagonist 1) is an antagonist of NK-1 receptor, used in the research of NK-1 related diseases and conditions such as cough, overactive bladder, alcohol dependency and depression .

HY-155487

JTE-151	ROR	Neurological Disease Inflammation/Immunology
JTE-151 is a RORγ inhibitor, which can suppress overactive immune response through inhibition of RORγ related to the activation of Th17 cells, making JTE-151 possible to be used in autoimmune disease research .

HY-14828

Afacifenacin SMP-986	mAChR	Metabolic Disease
Afacifenacin (SMP-986) is a potent and orally active muscarinic receptor antagonist. Afacifenacin inhibits the bladder afferent pathway through the sodium-channel blockade, increasing volume, and reducing the frequency of urination and incontinence. Afacifenacin has the potential for the research of overactive bladder (OAB) .

HY-100345

AMTB hydrochloride 1 Publications Verification
AMTB hydrochloride is a selective TRPM8 channel blocker. AMTB hydrochloride inhibits icilin-induced TRPM8 channel activation with a pIC₅₀ of 6.23. AMTB hydrochloride can be used for the research of the overactive bladder and painful bladder syndrome. AMTB hydrochloride is a non-selective inhibitor of voltage-gated sodium channels (Na_V) .

HY-19436

Solabegron 1 Publications Verification GW 427353	Adrenergic Receptor	Metabolic Disease Endocrinology
Solabegron (GW 427353) is a selective β₃-adrenergic receptor agonist, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β₃-AR, with an EC₅₀ value of 22 nM . Solabegron (GW 427353) is being developed for the treatment of overactive bladder and irritable bowel syndrome .

HY-B0461

Trospium chloride	mAChR	Neurological Disease
Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .

HY-109147

Imnopitant

Neurokinin Receptor Neurological Disease Endocrinology

Imnopitant is a NK1 receptor antagonist (WO2020132716, compound 1) .

Imnopitant	Neurokinin Receptor	Neurological Disease Endocrinology
Imnopitant is a NK1 receptor antagonist (WO2020132716, compound 1) .

HY-76569

Desfesoterodine PNU-200577; 5-Hydroxymethyl Tolterodine	mAChR	Neurological Disease
Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a K_B and a pA₂ of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .

HY-A0030S

Fesoterodine-d7 fumarate	mAChR
Fesoterodine-d₇ (fumarate) is the deuterium labeled Fesoterodine fumarate[1]. Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB)[2][3].

HY-100490

Rilmenidine	Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy	Cardiovascular Disease Cancer
Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na ⁺/H ⁺ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .

HY-100490B

Rilmenidine phosphate	Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy	Cardiovascular Disease Cancer
Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na ⁺/H ⁺ antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .

HY-100490A

Rilmenidine hemifumarate	Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy	Cardiovascular Disease Cancer
Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na ⁺/H ⁺ antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .

HY-147383

NS-8	Potassium Channel	Endocrinology
NS-8, a pyrrole derivative, activates the Ca ²⁺-sensitive k ⁺-channel. NS-8 can suppress the micturition reflex by decreasing afferent pelvic nerve activity. NS-8 can be used in the research of urinary frequency and incontinence .

HY-100490S

Rilmenidine-d4	Isotope-Labeled Compounds Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy	Cardiovascular Disease Cancer
Rilmenidine-d₄ is the deuterium labeled Rilmenidine. Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].

HY-76570S

(Rac)-5-Hydroxymethyl Tolterodine-d14 (Rac)-Desfesoterodine-d₁₄; (Rac)-PNU-200577-d₁₄	mAChR	Neurological Disease
(Rac)-5-Hydroxymethyl Tolterodine-d₁₄ is the deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research[1].

HY-76570S1

5-Hydroxymethyl Tolterodine-d14 formate	Isotope-Labeled Compounds mAChR	Neurological Disease
5-Hydroxymethyl Tolterodine-d₁₄ (formate) is deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research[1].

HY-B0267A

Oxybutynin chloride	mAChR Potassium Channel	Neurological Disease
Oxybutynin chloride is an oral active and competitive mAChR antagonist with K_is of 14.3 and 5.55 nM for specific [ ³H]NMS binding in the mouse bladder and cerebral cortex, respectively. Oxybutynin chloride inhibits vascular Kv channels in a manner independent of anticholinergic effect, with an IC₅₀ value of 11.51 μM. Oxybutynin chloride reduces muscle spasm in the bladder and urinary tract, can be used in study of overactive bladder syndrome (OAB) . Oxybutynin (chloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-B0267AR

Oxybutynin chloride (Standard)	mAChR Potassium Channel	Neurological Disease
Oxybutynin (chloride) (Standard) is the analytical standard of Oxybutynin (chloride). This product is intended for research and analytical applications. Oxybutynin chloride is an oral active and competitive mAChR antagonist with K_is of 14.3 and 5.55 nM for specific [ ³H]NMS binding in the mouse bladder and cerebral cortex, respectively. Oxybutynin chloride inhibits vascular Kv channels in a manner independent of anticholinergic effect, with an IC₅₀ value of 11.51 μM. Oxybutynin chloride reduces muscle spasm in the bladder and urinary tract, can be used in study of overactive bladder syndrome (OAB) . Oxybutynin (chloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-15416

NS309	Potassium Channel	Cardiovascular Disease Neurological Disease
NS309 is a potent and selective activator of the Ca ²⁺-activated SK/IK potassium channels, but displays no activity at BK channels .

Cat. No.	Product Name	Chemical Structure

HY-116408AS

Propiverine-d7 hydrochloride
Propiverine-d₇ (hydrochloride) is the deuterium labeled Propiverine hydrochloride. Propiverine hydrochloride is a bladder spasmolytic with calcium antagonistic and anticholinergic properties. Propiverine hydrochloride can be used for the research of overactive blaqdder and urinary incontinence[1][2].

HY-A0030S

Fesoterodine-d7 fumarate
Fesoterodine-d₇ (fumarate) is the deuterium labeled Fesoterodine fumarate[1]. Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB)[2][3].

HY-100490S

Rilmenidine-d4
Rilmenidine-d₄ is the deuterium labeled Rilmenidine. Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].

Rilmenidine-d4

Rilmenidine-d₄ is the deuterium labeled Rilmenidine. Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].

HY-76570S

(Rac)-5-Hydroxymethyl Tolterodine-d14
(Rac)-5-Hydroxymethyl Tolterodine-d₁₄ is the deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research[1].

(Rac)-5-Hydroxymethyl Tolterodine-d14

(Rac)-5-Hydroxymethyl Tolterodine-d₁₄ is the deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research[1].

HY-76570S1

5-Hydroxymethyl Tolterodine-d14 formate
5-Hydroxymethyl Tolterodine-d₁₄ (formate) is deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research[1].

5-Hydroxymethyl Tolterodine-d14 formate

5-Hydroxymethyl Tolterodine-d₁₄ (formate) is deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research[1].

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