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Results for "

overactive

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (3) Adenosine Receptor (5) Adrenergic Receptor (20) Akt (3) Amyloid-β (3) Apoptosis (8) Autophagy (7) Calcium Channel (11) Calmodulin (1) Carbonic Anhydrase (1) Cytochrome P450 (6) Dopamine Receptor (5) Drug Metabolite (1) FAAH (1) GABA Receptor (1) GnRH Receptor (1) iGluR (3) Imidazoline Receptor (7) Isotope-Labeled Compounds (12) mAChR (44) MCHR1 (GPR24) (1) mTOR (3) Neurokinin Receptor (2) Nucleoside Transporters (1) Opioid Receptor (2) P2X Receptor (1) p38 MAPK (3) Potassium Channel (8) PPAR (1) Prostaglandin Receptor (2) Reference Standards (16) ROR (1) Tau Protein (3) TRP Channel (2) Vasopressin Receptor (2)
By Research Areas:	Cancer (29) Cardiovascular Disease (11) Endocrinology (14) Infection (2) Inflammation/Immunology (5) Metabolic Disease (24) Neurological Disease (58)

By Targets:

5-HT Receptor (3)

Adenosine Receptor (5)

Adrenergic Receptor (20)

Akt (3)

Amyloid-β (3)

Apoptosis (8)

Autophagy (7)

Calcium Channel (11)

Calmodulin (1)

Carbonic Anhydrase (1)

Cytochrome P450 (6)

Dopamine Receptor (5)

Drug Metabolite (1)

FAAH (1)

GABA Receptor (1)

GnRH Receptor (1)

iGluR (3)

Imidazoline Receptor (7)

Isotope-Labeled Compounds (12)

mAChR (44)

MCHR1 (GPR24) (1)

mTOR (3)

Neurokinin Receptor (2)

Nucleoside Transporters (1)

Opioid Receptor (2)

P2X Receptor (1)

p38 MAPK (3)

Potassium Channel (8)

PPAR (1)

Prostaglandin Receptor (2)

Reference Standards (16)

ROR (1)

Tau Protein (3)

TRP Channel (2)

Vasopressin Receptor (2)

By Research Areas:

Cancer (29)

Cardiovascular Disease (11)

Endocrinology (14)

Infection (2)

Inflammation/Immunology (5)

Metabolic Disease (24)

Neurological Disease (58)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-A0033

Darifenacin Maximum Cited Publications 7 Publications Verification UK-88525	mAChR p38 MAPK Akt	Neurological Disease Metabolic Disease Cancer
Darifenacin (UK-88525) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin inhibits tumor growth in colorectal cancer cells and has anti-tumor effects .

HY-A0012

Darifenacin hydrobromide Maximum Cited Publications 7 Publications Verification UK-88525 hydrobromide	mAChR p38 MAPK Akt	Neurological Disease Metabolic Disease Cancer
Darifenacin (UK-88525) hydrobromide is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin hydrobromide binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin hydrobromide can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin hydrobromide inhibits tumor growth in colorectal cancer cells and has anti-tumor effects .

HY-19933

Vibegron 1 Publications Verification 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-A0030

Fesoterodine fumarate	mAChR	Neurological Disease Metabolic Disease Cancer
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-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-B0549A

Flavoxate hydrochloride Rec-7-0040; DW61	Calcium Channel Adenosine Receptor mAChR Dopamine Receptor Adrenergic Receptor	Cardiovascular Disease Infection Neurological Disease Cancer
Flavoxate hydrochloride (Rec-7-0040; DW61) is an orally active L-type Ca ²⁺ channel inhibitor and antispasmodic. Flavoxate hydrochloride inhibits cyclic adenosine monophosphate production by blocking voltage-dependent inward Ba ²⁺ currents, regulating the brainstem micturition center, and stimulating G protein-coupled receptors. Consequently, Flavoxate hydrochloride induces relaxation of bladder smooth muscle and inhibits isovolumetric rhythmic contractions. Flavoxate hydrochloride effectively increases bladder capacity and alleviates symptoms of urgent urination frequency and pollakiuria caused by overactive bladder. Flavoxate hydrochloride can be used in research on overactive bladder and related voiding dysfunctions .

HY-76569

Desfesoterodine 1 Publications Verification PNU-200577; 5-Hydroxymethyl Tolterodine	mAChR	Neurological Disease Cancer
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-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-B0267A

Oxybutynin chloride	mAChR Potassium Channel	Neurological Disease Cancer
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 .

HY-100345

AMTB hydrochloride 2 Publications Verification	TRP Channel	Neurological Disease Cancer
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-139142

Simufilam 1 Publications Verification PTI-125	mTOR iGluR Amyloid-β Tau Protein	Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Simufilam (PTI-125) is an orally active FLNA modulator. Simufilam restores NMDAR signaling and Arc expression. Simufilam inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, improves insulin sensitivity, reduces Aβ₄₂-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam can be used for research of Alzheimer's disease .

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-A0024

Tolterodine (R)-(+)-Tolterodine; (+)-Tolterodine; (R)-Tolterodine; PNU-200583	mAChR Cytochrome P450	Neurological Disease Cancer
Tolterodine ((R)-(+)-Tolterodine) is a mAChR inhibitor and substrate for cytochrome P450 enzymes. Tolterodine competitively binds acetylcholine, reduces sympathetic excitation, and inhibits involuntary bladder muscle contraction. Tolterodine restores the Nrf2/NF-κB signaling pathway, mediates protection against inflammatory response and ferroptosis. Tolterodine ameliorates LPS (HY-D1056)-induced reactive oxygen species production and lipid oxidation. Tolterodine can be used for the research of urinary tract infections and overactive bladder .

HY-90010

Tolterodine tartrate Kabi-2234; PNU-200583E	mAChR Cytochrome P450	Neurological Disease Cancer
Tolterodine tartrate (Kabi-2234) is a mAChR inhibitor and substrate for cytochrome P450 enzymes. Tolterodine tartrate competitively binds acetylcholine, reduces sympathetic excitation, and inhibits involuntary bladder muscle contraction. Tolterodine tartrate restores the Nrf2/NF-κB signaling pathway, mediates protection against inflammatory response and ferroptosis. Tolterodine tartrate ameliorates LPS (HY-D1056)-induced reactive oxygen species production and lipid oxidation. Tolterodine tartrate can be used for the research of urinary tract infections and overactive bladder .

HY-116408A

Propiverine hydrochloride	mAChR Calcium Channel	Neurological Disease Cancer
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-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-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-15574

Piboserod 4 Publications Verification SB-207266	5-HT Receptor	Cardiovascular Disease
Piboserod is an orally available selective antagonist of the 5-HT4 receptor, with a K_i value of approximately 0.1 nM for human 5-HT4 receptors. Piboserod can competitively bind to the 5-HT4 receptor and block the activation of the 5-HT4 receptor. Piboserod can inhibit the enhancing effect of 5-HT on the nerve-mediated contraction response of the human bladder detrusor muscle. Piboserod is mainly used in the research of urinary system diseases (such as overactive bladder) and cardiovascular diseases (such as chronic heart failure) .

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-B0662

Imidafenacin KRP-197; ONO-8025	mAChR Vasopressin Receptor	Neurological Disease Endocrinology
Imidafenacin (KRP-197; ONO-8025) is an orally active inhibitor of muscarinic (mAChR) M₁ and M₃ receptors. Imidafenacin potently inhibits bladder contraction in vivo and exerts an antidiuretic effect by enhancing the signaling pathway of vasopressin (antidiuretic hormone). Imidafenacin can be used in research related to overactive bladder .

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-118301

ADX71441	GABA Receptor 5-HT Receptor	Neurological Disease
ADX71441 is an orally active, blood-brain barrier penetrant positive allosteric modulator of GABA_B receptor. ADX71441 potentiates the activity of endogenous GABA at GABA_B receptor, with an EC₅₀ of 96 nM. ADX71441 functionally inhibits adenosine transporters and 5-HT_2B receptor. ADX71441 produces anxiolytic-like, analgesic, muscle relaxant, hypothermic and overactive bladder inhibitory effects, reduces acute locomotor activity levels, decreases voluntary intake of alcohol and saccharin, attenuates stress-induced neuronal activation, and exhibits anti-hyperalgesic activity .

HY-109532

Ganirelix acetate Ganirest	GnRH Receptor	Metabolic Disease
Ganirelix acetate (Ganirest) is a competitive and selective gonadotropin-releasing hormone (GnRH) antagonist. Ganirelix acetate blocks endogenous GnRH-induced release of luteinizing hormone (LH) and follicle-stimulating hormone. Ganirelix acetate antagonizes Prostaglandin E2 (HY-101952)-induced detrusor overactivity and enhances Carbachol (HY-B1208)-induced detrusor contraction. Ganirelix acetate is applicable to research related to female infertility and detrusor overactivity .

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-139142B

Simufilam hydrochloride 1 Publications Verification PTI-125 hydrochloride	mTOR iGluR Amyloid-β Tau Protein	Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Simufilam hydrochloride (PTI-125 hydrochloride) is an orally active FLNA modulator. Simufilam hydrochloride restores NMDAR signaling and Arc expression. Simufilam hydrochloride inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, improves insulin sensitivity, reduces Aβ₄₂-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam hydrochloride can be used for research of Alzheimer's disease .

HY-W074975

CL 5343 5-Amino-1,3,4-thiadiazole-2-sulfonamide	Carbonic Anhydrase	Cancer
CL 5343 (5-Amino-1,3,4-thiadiazole-2-sulfonamide) is a selective inhibitor of carbonic anhydrase B (HCA-B) and isoforms I, II, IV, and VII. CL 5343 has a K_i of 7.9 nM for hCA II. CL 5343 acts as a CA9 ligand to achieve targeted delivery of maytansine to the cell membrane of SKRC52 renal cancer cells. CL 5343 is useful in the development of therapeutics for diseases associated with CA overactivity, such as glaucoma, epilepsy, and cancer .

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-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-139583

Sunobinop S 117957; IMB 115	Opioid Receptor	Neurological Disease
Sunobinop (S 117957; IMB 115) is an orally active and blood-brain barrier-permeable selective partial agonist of the human nociceptin/orphanin FQ receptor (NOP), which exhibits high affinity for human targets (K_i=3.3 nM; EC₅₀=4.03 nM; E_max=47.8%) without activating μ and κ opioid receptors. Sunobinop significantly reduces wakefulness time and increases non-rapid eye movement sleep in rats by activating NOP receptors, and produces no significant side effects on learning, memory, reward, respiration or intestinal function at effective doses. Sunobinop displays competitive antagonist properties in specific signaling pathways, such as β-arrestin 2 recruitment. With these unique pharmacological properties, Sunobinop can be used to investigate insomnia, moderate-to-severe alcohol use disorder, and urinary incontinence caused by overactive bladder .

HY-B0461R

Trospium chloride (Standard)	mAChR Reference Standards	Neurological Disease
Trospium (chloride) (Standard) is the analytical standard of Trospium (chloride). This product is intended for research and analytical applications. 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-70053A

Fesoterodine L-mandelate	mAChR	Neurological Disease Metabolic Disease Cancer
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-116927

KW-7158	Nucleoside Transporters Apoptosis	Neurological Disease
KW-7158 is a putative afferent nerve inhibitor that can depress vesica-vascular reflexes in rats. KW-7158 is an inhibitor of nucleoside transporter-1 (ENT1/SLC29A1) and acts as an antagonist for overactive bladder (OAB) .

HY-139142A

Simufilam dihydrochloride PTI-125 dihydrochloride	Tau Protein Amyloid-β mTOR iGluR	Neurological Disease
Simufilam dihydrochloride (PTI-125 dihydrochloride) is an orally active FLNA modulator. Simufilam dihydrochloride restores NMDAR signaling and Arc expression. Simufilam dihydrochloride inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, improves insulin sensitivity, reduces Aβ₄₂-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam dihydrochloride can be used for research of Alzheimer's disease .

HY-B0549

Flavoxate Rec-7-0040 free base; DW61 free base	mAChR Calcium Channel Adrenergic Receptor Adenosine Receptor Dopamine Receptor	Neurological Disease
Flavoxate (Rec-7-0040 free base; DW61 free base) is an orally active L-type Ca ²⁺ channel inhibitor and antispasmodic. Flavoxate inhibits cyclic adenosine monophosphate production by blocking voltage-dependent inward Ba ²⁺ currents, regulating the brainstem micturition center, and stimulating G protein-coupled receptors. Consequently, Flavoxate induces relaxation of bladder smooth muscle and inhibits isovolumetric rhythmic contractions. Flavoxate effectively increases bladder capacity and alleviates symptoms of urgent urination frequency and pollakiuria caused by overactive bladder. Flavoxate can be used in research on overactive bladder and related voiding dysfunctions .

HY-B0549AR

Flavoxate hydrochloride (Standard) Rec-7-0040 (Standard); DW61 (Standard)	Reference Standards mAChR Calcium Channel Adrenergic Receptor Adenosine Receptor Dopamine Receptor	Neurological Disease
Flavoxate (hydrochloride) (Standard) is the analytical standard of Flavoxate (hydrochloride). This product is intended for research and analytical applications. Flavoxate hydrochloride (Rec-7-0040; DW61) is an orally active L-type Ca ²⁺ channel inhibitor and antispasmodic. Flavoxate hydrochloride inhibits cyclic adenosine monophosphate production by blocking voltage-dependent inward Ba ²⁺ currents, regulating the brainstem micturition center, and stimulating G protein-coupled receptors. Consequently, Flavoxate hydrochloride induces relaxation of bladder smooth muscle and inhibits isovolumetric rhythmic contractions. Flavoxate hydrochloride effectively increases bladder capacity and alleviates symptoms of urgent urination frequency and pollakiuria caused by overactive bladder. Flavoxate hydrochloride can be used in research on overactive bladder and related voiding dysfunctions .

HY-A0030S

Fesoterodine-d7 fumarate	mAChR	Metabolic Disease
Fesoterodine-d₇ (fumarate) is the deuterium labeled Fesoterodine fumarate . 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) .

HY-W039283

MCH-1 antagonist 2	MCHR1 (GPR24)	Neurological Disease Cancer
MCH-1 antagonist 2 (l-BROMO-2,4-DIFLUORO-5-NITROBEN-ZENE) is a melanin concentrating hormone-1 (MCH1) receptor-selective 4-aryl piperidine. MCH-1 antagonist 2 can be used for the research of depression, anxiety, obesity, urge incontinence, urinary incontinence, major depression, bipolar disorder, agoraphobia, specific phobia, social phobia, obsessive-compulsive disorder, post-traumatic stress disorder, acute stress disorder, urinary frequency, urinary urgency, nocturia, enuresis, bulimia, bulimia nervosa, anorexia nervosa, major depressive disorder, dysthymic disorder, bipolar 1 and 2 disorders, schizoaffective disorder, cognitive disorders with depressed mood, personality disorders, insomnia, hypersomnia, narcolepsy, circadian rhythm sleep disorder, nightmare disorder, sleep terror disorder, sleepwalking disorder, panic disorder, social anxiety disorder, generalized anxiety disorder, overactive bladder .

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 .

HY-19116

KRN-2391	Potassium Channel	Neurological Disease Metabolic Disease
KRN-2391 is a K_ATP channel opener with NO donor properties. KRN-2391 exerts dual inhibitory effects on overactive bladder (OAB) by activating KATP channels (causing cellular hyperpolarization and bladder smooth muscle relaxation) and releasing NO (enhancing relaxation via cGMP pathways). KRN-2391 is promising for research of OAB .

HY-76569R

Desfesoterodine (Standard) PNU-200577 (Standard); 5-Hydroxymethyl Tolterodine (Standard)	Reference Standards mAChR	Neurological Disease
Desfesoterodine (Standard) is the analytical standard of Desfesoterodine. This product is intended for research and analytical applications. 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-120473

TAK-259	Adrenergic Receptor	Metabolic Disease
TAK-259 is an orally active α1D-adrenergic receptor antagonist with a K_i value of 1.1 nM for human α1D-adrenergic receptors. TAK-259 can inhibit the contraction of isolated bladder strips in rats with bladder outlet obstruction, reduce non-voiding bladder contractions, and improve urinary frequency symptoms. TAK-259 can be used in research related to overactive bladder .

HY-117372

DFL23448	TRP Channel	Metabolic Disease
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 .

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-106415

Terflavoxate	Calcium Channel	Neurological Disease
Terflavoxate is a flavone derivative with spasmolytic properties. Terflavoxate has Ca ²⁺-antagonistic effect is mainly responsible for Terflavoxate smooth muscle relaxant properties. Terflavoxate has the potential for overactive detrusor research .

HY-123566

PSD-506 RO 3202904	mAChR	Metabolic Disease
PSD-506 (RO 3202904) is a muscarinic M2/M3 antagonist. PSD-506 has the potential to be used in studies of bladder overactivity and urinary incontinence .

HY-171843

TD-6301	mAChR	Endocrinology
TD-6301 is a bladder-selective M_2/4 muscarinic receptor antagonist. TD-6301 binds to and blocks M_2/4 muscarinic receptors with high selectivity, especially human M₂ receptors with strong affinity (K_i = 0.36 nM). TD-6301 inhibits volume-induced bladder contractions (ID₅₀ = 0.075 mg/kg). TD-6301 can be used in the research of overactive bladder .

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-116408AR

Propiverine hydrochloride (Standard)	Reference Standards mAChR Calcium Channel	Neurological Disease Cancer
Propiverine (hydrochloride) (Standard) is the analytical standard of Propiverine (hydrochloride). This product is intended for research and analytical applications. 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-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.

Cat. No.	Product Name	Chemical Structure

HY-A0030S

Fesoterodine-d7 fumarate
Fesoterodine-d₇ (fumarate) is the deuterium labeled Fesoterodine fumarate . 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) .

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 .

HY-B0549S

Flavoxate-d5

Flavoxate-d₅ is deuterium labeled Flavoxate. Flavoxate hydrochloride (Rec-7-0040; DW61) is an orally active L-type Ca ²⁺ channel inhibitor and antispasmodic. Flavoxate hydrochloride inhibits cyclic adenosine monophosphate production by blocking voltage-dependent inward Ba ²⁺ currents, regulating the brainstem micturition center, and stimulating G protein-coupled receptors. Consequently, Flavoxate hydrochloride induces relaxation of bladder smooth muscle and inhibits isovolumetric rhythmic contractions. Flavoxate hydrochloride effectively increases bladder capacity and alleviates symptoms of urgent urination frequency and pollakiuria caused by overactive bladder. Flavoxate hydrochloride can be used in research on overactive bladder and related voiding dysfunctions .

HY-B0549AS

Flavoxate-d4 hydrochloride

Flavoxate-d₄ hydrochloride (Rec-7-0040-d₄) is the deuterium labeled Flavoxate hydrochloride. Flavoxate hydrochloride (Rec-7-0040; DW61) is an orally active L-type Ca ²⁺ channel inhibitor and antispasmodic. Flavoxate hydrochloride inhibits cyclic adenosine monophosphate production by blocking voltage-dependent inward Ba ²⁺ currents, regulating the brainstem micturition center, and stimulating G protein-coupled receptors. Consequently, Flavoxate hydrochloride induces relaxation of bladder smooth muscle and inhibits isovolumetric rhythmic contractions. Flavoxate hydrochloride effectively increases bladder capacity and alleviates symptoms of urgent urination frequency and pollakiuria caused by overactive bladder. Flavoxate hydrochloride can be used in research on overactive bladder and related voiding dysfunctions .

HY-70053S

rac-Fesoterodine-d14 fumarate
(Rac)-Fesoterodine-d₁₄ fumarate is a labelled racemic Fesoterodine. Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK_ivalues 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-W720879

Fesoterodine-d3
Fesoterodine-d₃ is the deuterium labeled Fesoterodine (HY-70053). Fesoterodine 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 is used for the overactive bladder (OAB) .

HY-19436S

Solabegron-d8
Solabegron-d₈ (GW 427353-d₈) is deuterium labeled Solabegron. 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-76569S1

(R)-Hydroxytolterodine-d14

(R)-Hydroxytolterodine-d₁₄ is deuterated labeled Desfesoterodine (HY-76569). 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-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 .

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 .

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 .

HY-A0024S

Tolterodine-d14 hydrochloride

Tolterodine-d₁₄ (hydrochloride) is the deuterium labeled Tolterodine hydrochloride . Tolterodine ((R)-(+)-Tolterodine) is a mAChR inhibitor and substrate for cytochrome P450 enzymes. Tolterodine competitively binds acetylcholine, reduces sympathetic excitation, and inhibits involuntary bladder muscle contraction. Tolterodine restores the Nrf2/NF-κB signaling pathway, mediates protection against inflammatory response and ferroptosis. Tolterodine ameliorates LPS (HY-D1056)-induced reactive oxygen species production and lipid oxidation. Tolterodine can be used for the research of urinary tract infections and overactive bladder.

HY-90010S

Tolterodine tartrate-d14

Tolterodine tartrate-d₁₄ (Kabi-2234-d₁₄) is deuterium labeled Tolterodine tartrate. Tolterodine ((R)-(+)-Tolterodine) is a mAChR inhibitor and substrate for cytochrome P450 enzymes. Tolterodine competitively binds acetylcholine, reduces sympathetic excitation, and inhibits involuntary bladder muscle contraction. Tolterodine restores the Nrf2/NF-κB signaling pathway, mediates protection against inflammatory response and ferroptosis. Tolterodine ameliorates LPS (HY-D1056)-induced reactive oxygen species production and lipid oxidation. Tolterodine can be used for the research of urinary tract infections and overactive bladder.

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