bladder

Rosiglitazone (BRL49653) is a PPARγ agonist, TRPC5 activator, and TRPM3 inhibitor with oral activity. Rosiglitazone is also a hypoglycemic agent and a thiazolidinedione insulin sensitizer.

Tolterodine tartrate (PNU-200583E) is a potent antagonist for muscarinic receptor. It show selectivity for the urinary bladder and salivary glands in vivo.

Terazosin hydrochloride (Hytrin) , a selective alpha1-antagonist, can treat the benign prostatic hyperplasia (BPH). It also can lower blood pressure, so it is a drug of choice for patients with prostate enlargement and hypertension. It works on the smooth muscle of the bladder and the blood vessel walls by blocking the function of adrenaline.

Propantheline bromide (Pro-Banthine) competitively antagonizes acetylcholine activity mediated by muscarinic receptors at neuroeffector sites on smooth muscle and exocrine gland cells. Propantheline Bromide is the bromide salt form of propantheline, a quaternary ammonium compound structurally related to belladonna alkaloids. An aspartic acid residue present in the N-terminal portion of the third transmembrane helix of the muscarinic receptor is believed to form an ionic bond with the tertiary or quaternary nitrogen of the antagonist. Antagonism leads to a reduction of exocrine glands secretions and to relax the bronchial muscle and reduce tone and motility of intestinal smooth muscle.

Trospium chloride (Spasmex) is an antispasmodic and anticholinergic agent used to treat urinary incontinence and overactive bladder syndrome. Trospium chloride has not been implicated in causing liver enzyme elevations or clinically apparent acute liver injury.

Fesoterodine fumarate (Toviaz) is the fumarate salt form of fesoterodine, a competitive muscarinic receptor antagonist with muscle relaxant and urinary antispasmodic properties. Fesoterodine is rapidly hydrolyzed in vivo into its active metabolite 5-hydroxymethyl tolterodine, which binds and inhibits muscarinic receptors on the bladder detrusor muscle, thereby preventing bladder contractions or spasms caused by acetylcholine.

Rosiglitazone hydrochloride (BRL-49653 HCl) is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.

Cesium chloride (CsCl) is considered to be the most toxic of the alkali chlorides, inhibiting fungal growth.

CU-T12-9 is a potent TLR1/2 agonist(EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay). It acts by activating the NFkB pathway, upregulating proinflammatory cytokines, and enhancing TLR1 and TLR2 dimerization.CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.

AMTB hydrochloride (AMTB HCl) is a novel TRPM8 channel blocker and is effective for pain and urinary diseases. AMTB can act on the bladder afferent pathway to attenuate the bladder micturition reflex and nociceptive reflex responses in the rat.

NS309 is a nonselective activator of small- and intermediate-conductance Ca2+-activated K+ (SK/KCa2 and IK/KCa3.1) channels (EC50s range from 0.12-1.2 µM for SK channels and 10-90 nM for IK channels). It can also activate voltage-gated Kv11.1 channels (hE

Propiverine is a widely used antimuscarinic drug with a mixed mode of action in the treatment of symptoms associated with overactive bladder (OAB).

Terazosin hydrochloride dihydrate (Heitrin dihydrate) is a selective α1-adrenoceptor antagonist, used for treatment of symptoms of an enlarged prostate (BPH).

Fesoterodine ((R) Fesoterodine) is an orally active, competitive mAChR antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. It is used for the overactive bladder (OAB).

Cyclophosphamide is an alkylating agent type of anti-tumor drug, and its main target is DNA. Cyclophosphamide inhibits the proliferation of tumor cells by undergoing alkylation reactions with DNA, interfering with the replication and transcription processes of DNA.

1-Methyluric acid (1-Methylurate) acts on the bladder mucosa and increases the levels of insulin, triglycerides, cholesterol, and blood glucose.

MK-8033 hydrochloride is an effective and orally active dual inhibitor of ATP competitive c-Met/Ron, with 1 nM for c-Met and 7nM for Ron IC50. MK-8033 hydrochloride has a high affinity for activated kinase conformation, and is suitable for the study of breast cancer, bladder cancer, and non-small cell lung cancer (NSCLC).

Stilbamidine (Ba 2652) has antifungal and anticancer activity and can be used to study multiple myeloma and bladder migratory cell carcinoma.

CID-5056270 has anticancer activity and can inhibit lung cancer, anal cancer, bladder cancer, cervical cancer, vulvar cancer, penile cancer, Burkitt's lymphoma, breast cancer and bone cancer. It can be used to study hypertension, Alzheimer's disease and arteriosclerosis.

Bencycloquidium Bromide is a muscarinic M3 antagonist. Bencycloquidium bromide inhibits nasal hypersecretion in a rat model of allergic rhinitis. Bencycloquidium Bromide showed high affinity toward the M(3) receptor in Chinese hamster ovary (CHO) cells (M(1) pKi=7.86, M(2) pKi=7.21, M(3) pKi=8.21); pA(2)=8.85, 8.71 and 8.57 in methacholine-induced contraction of trachea, ileum and urinary bladder, 8.19 in methacholine-induced bradycardia of right atrium in vitro, respectively.This compound is unstable in powder form and other related salt forms are recommended.

N-5984, a β3-adrenergic receptor agonist, is used potentially for the treatment of obesity, overactive bladder and type 2 diabetes.

Ritobegron (KUC-7483), an effective and selective β3-adrenergic receptor agonist, shows effective β(3)-AR agonist activity on transfected human β-AR and has an effect on the bladder of rats Shows high selectivity with other organs.

MS8511, a selective covalent irreversible inhibitor of G9a/GLP, targets a cysteine residue at the substrate binding site, displaying IC50 values of 100 nM (G9a) and 140 nM (GLP), alongside Kd values of 44 nM (G9a) and 46 nM (GLP). This compound effectively reduces cellular H3K9me2 levels and boosts antiproliferation activity, making it applicable in cancer research involving brain, breast, ovarian, lung, bladder, melanoma, and colorectal cancers, as well as studies on Alzheimer's disease (AD), sickle cell disease, and Prader−Willi syndrome (PWS) [1].

mTOR/HDAC-IN-1 (Compound 50) is a dual inhibitor of mTOR and HDAC, with IC50 values of 0.49 nM and 0.91 nM, respectively, holding potential as an anti-cancer agent [1].