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41

Inhibitors & Agonists

6

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 .
    Propiverine hydrochloride
  • 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 (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 .
    (Rac)-5-Hydroxymethyl Tolterodine
  • 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 .
    Vibegron
  • 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 pKi of 8.3. EP3 antagonist 3 shows excellent pharmacokinetic properties. EP3 antagonist 3 can be used for overactive bladder (OAB) research .
    EP3 antagonist 3
  • 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 .
    Flavoxate hydrochloride
  • 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 .
    Propiverine
  • 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 .
    Oleoyl ethyl amide
  • 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 .
    Terflavoxate
  • 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 (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 hydrochloride can be used for overactive bladder research .
    (Rac)-5-Hydroxymethyl Tolterodine hydrochloride
  • 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 .
    Flavoxate
  • HY-B0549AR
    Flavoxate hydrochloride (Standard)

    		Phosphodiesterase (PDE) Calcium Channel mAChR Neurological Disease
    Flavoxate (hydrochloride) (Standard) is the analytical standard of Flavoxate (hydrochloride). This product is intended for research and analytical applications. 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 .
    Flavoxate hydrochloride (Standard)
  • HY-100345
    AMTB hydrochloride
    1 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 (NaV) .
    AMTB hydrochloride
  • 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 α1D-adrenoceptor (α1D-AR) antagonist (Ki=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.
    ADRA1D receptor antagonist 1 free base
  • HY-A0030
    Fesoterodine fumarate

    		mAChR Neurological Disease Metabolic Disease
    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) .
    Fesoterodine fumarate
  • HY-70053
    Fesoterodine

    		mAChR Neurological Disease Metabolic Disease
    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) .
    Fesoterodine
  • 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 pKi 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) .
    Fesoterodine L-mandelate
  • 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 .
    BAY-9683
  • 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].
    Propiverine-d7 hydrochloride
  • 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 .
    SCH 900978
  • 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 .
    JTE-151
  • 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) .
    Afacifenacin
  • HY-19436A
    Solabegron hydrochloride

    GW 427353B

    		 Adrenergic Receptor Metabolic Disease Endocrinology
    Solabegron hydrochloride 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 hydrochloride (GW 427353) is being developed for the treatment of overactive bladder and irritable bowel syndrome .
    Solabegron hydrochloride
  • 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 .
    Trospium chloride
  • HY-109147
    Imnopitant

    		Neurokinin Receptor Neurological Disease Endocrinology
    Imnopitant is a NK1 receptor antagonist (WO2020132716, compound 1) .
    Imnopitant
  • HY-B0461R
    Trospium chloride (Standard)

    		mAChR 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 .
    Trospium chloride (Standard)
  • 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 .
    Solabegron
  • 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 KB 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 .
    Desfesoterodine
  • HY-A0030S
    Fesoterodine-d7 fumarate

    		mAChR Metabolic Disease
    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].
    Fesoterodine-d7 fumarate
  • 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 .
    Rilmenidine
  • 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 .
    Rilmenidine phosphate
  • 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 .
    Rilmenidine hemifumarate
  • HY-76569S1
    (R)-Hydroxytolterodine-d14

    PNU-200577-d14; 5-Hydroxymethyl Tolterodine-d14

    		 mAChR Isotope-Labeled Compounds Neurological Disease
    (R)-Hydroxytolterodine-d14 is deuterated labeled Desfesoterodine (HY-76569). Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB 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 .
    (R)-Hydroxytolterodine-d14
  • HY-76569R
    Desfesoterodine (Standard)

    		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 KB 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 .
    Desfesoterodine (Standard)
  • 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 .
    NS-8
  • 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].
    Rilmenidine-d4
  • 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].
    (Rac)-5-Hydroxymethyl Tolterodine-d14
  • 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].
    5-Hydroxymethyl Tolterodine-d14 formate
  • HY-120158
    ZD0947

    		Others Neurological Disease
    ZD0947 is an ATP-sensitive potassium channel activator with relatively effective activation of smooth muscle KATP channels (SUR2B/Kir6.1 and SUR2B/Kir6.2). ZD0947 partially antagonizes pancreatic KATP channels (SUR1/Kir6.2) and cardiac KATP channels (SUR2A/Kir6.2). ZD0947 is potentially used to inhibit overactive bladder (OAB) .
    ZD0947
  • HY-B0267A
    Oxybutynin chloride

    		mAChR Potassium Channel Neurological Disease
    Oxybutynin chloride is an oral active and competitive mAChR antagonist with Kis 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.
    Oxybutynin chloride
  • 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 Kis 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.
    Oxybutynin chloride (Standard)
  • 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 .
    NS309

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