luminal

Dinoprost (Prostaglandin F2a) 是口服有效的、内源性的前列腺素 F 受体激动剂。它是在子宫内膜腔上皮和黄体中局部产生的溶酶激素。它在分娩过程中起关键作用。

Dinoprost tromethamine salt (PGF2α THAM) 是一种口服有效的前列腺素 F 受体激动剂。它是在子宫内膜腔上皮和黄体中局部产生的溶酶激素，在分娩过程中起关键作用。

Tiliquinol (NSC-130828) 是一种与tibroquinol经常联用、具有抗阿米巴特性的非吸收性腔内药物，通常用于研究和调查阿米巴性肝脓肿。

Amiloride hydrochloride dihydrate (Amiloride HCl dihydrate) 是上皮钠通道 (ENaC) 和尿激酶型纤溶酶原激活物受体 (uTPA) 的抑制剂。它是polycystin-2 通道阻断剂。

Ilaprazole sodium (IY-81149 sodium) 是一种具有口服活性质子泵抑制剂，以剂量依赖性方式不可逆地抑制 H+ K+-ATPase，在兔壁细胞制剂中的 IC50为 6 μM。它也是一种有效的 T 细胞起源蛋白激酶(TOPK)抑制剂，用于胃溃疡的研究。

Diloxanide (RD3803) 是一种抗原虫制剂，可研究组织学内阿米巴原虫或者其他原虫感染引起的无症状肠道阿米巴病。它是一种活性的鲁米那抗阿米巴试剂，是由其前药二氯尼特糠酸酯在胃肠道中水解得来的。

BACE-IN-1 acetate (BACE-IN-1 acetate (350228-37-4，Free base)) 已被用作 BACE1 抑制剂测定中的 β 位淀粉样前体蛋白 (APP) 裂解酶-1 (BACE1) 抑制剂。 β-位点淀粉样前体蛋白 (APP) 切割酶-1 (BACE1)是一种天冬氨酸蛋白酶，属于蛋白酶家族，由六个腔内半胱氨酸残基组成。这些残基有助于形成三个分子间二硫键和 N-连接的糖基化位点。

Olsalazine-13C6is intended for use as an internal standard for the quantification of olsalazine by GC- or LC-MS. Olsalazine is an orally bioavailable prodrug form of the anti-inflammatory agent 5-aminosalicylic acid that is cleaved by bacterial azo reductases in the gut to generate active 5-ASA.1In vitro, olsalazine increases ion transport in isolated rabbit distal ileum when applied to the luminal side (ED50= 0.3 mM) and stimulates fluid transport in rat jejunum when used at a concentration of 5 mM.2,3Olsalazine (150 mg/kg for 8 days) improves stool consistency and decreases occult and gross bleeding as well as myeloperoxidase (MPO) activity and leukotriene B4levels in colon tissue in a mouse model of acute colitis induced by dextran sulfate .4Olsalazine also inhibits bovine xanthine oxidasein vitro(IC50= 3.4 mg/L) and lowers serum uric acid levels in a mouse model of hyperuricemia induced by oxonic acid when administered at a dose of 20 mg/kg.5Formulations containing olsalazine have been used in the treatment of inflammatory bowel disease (IBD) and ulcerative colitis. 1.Nugent, S.G., Kumar, D., Rampton, D.S., et al.Intestinal luminal pH in inflammatory bowel disease: Possible determinants and implications for therapy with aminosalicylates and other drugsGut48(4)571-577(2001) 2.Pamukcu, R., Hanauer, S.B., and Chang, E.B.Effect of disodium azodisalicylate on electrolyte transport in rabbit ileum and colon in vitro. Comparison with sulfasalazine and 5-aminosalicylic acidGastroenterology95(4)975-981(1988) 3.Mohsen, A.Q.M., Mulvey, D., Priddle, J.D., et al.Effects of olsalazine in the jejunum of the ratGut28(3)346-352(1987) 4.Murthy, S., Murthy, N.S., Coppola, D., et al.The efficacy of BAY y 1015 in dextran sulfate model of mouse colitisInflamm. Res.46(6)224-233(1997) 5.Niu, Y., Li, H., Gao, L., et al.Old drug, new indication: Olsalazine sodium reduced serum uric acid levels in mice via inhibiting xanthine oxidoreductase activityJ. Pharmacol. Sci.135(3)114-120(2017)

The growth factors, platelet-derived growth factor (PDGF) and basic fibroblast growth factor (bFGF) play major roles in enhanced smooth muscle cells growth in rodent blood vessels after vascular injury. Tyrosine kinase inhibition has been shown to be effective in blocking tyrosine phosphorylation at the PDGF and bFGF receptors in cultured fibroblast and vascular smooth muscle cells which in turn inhibits their proliferation[1]. CGP 53716 is a specific PDGFR tyrosine kinase inhibitor on SMC (smooth muscle cell) proliferation and migration in vitro and in neointimal formationin vivo[3]. CGP 53716 inhibited serum-induced cell growth in RASMC (rat aortic smooth muscle cells). And it completely blocked PDGF-BB tyrosine receptor autophosphorylation in RASMC and 3T3 cells, PDGF-BB-induced phosphorylation of mitogen-activated protein kinase at 1 μM in RASMC and inhibited PDGF-BB-induced c-Fos protein expression at 1 μM in RASMC; consistent with inhibition of PDGF-BB-induced DNA synthesis. Further, CGP 53716 inhibited PDGF-BB-, bFGF- and EGF-induced DNA synthesis in a concentration-dependent manner in each cell line. And it showed a 2- to 4-fold selectivity for PDGF-BB-stimulated DNA synthesis over bFGF or EGF in RASMC or 3T3 cells[1]. CGP 53716 inhibited dose dependently tyrosine phosphorylation of both the known PDGFRs: the PDGFR-α and PDGFR-β. After rat carotid artery ballooning injuryin vivo, the migration of alpha-actin-positive cells on the luminal side of internal elastic lamina was decreased with 50 mg kg day of CGP 53716 from 38 ± 10 (control group) to 4 ± 2. Intima media ratio was inhibited by 40% after 14 days in the CGP 53716-treated group (P=0.028) after rat aortic denudation[3].

NAA-004, also known as APAZA, has been shown to significantly inhibit toxin A-induced myeloperoxidase activity, luminal fluid accumulation, and structural damage to the colon in instances of toxin A-induced colitis.

BAY-5094是一种口服活性的PPAR gamma (PPARG) 反向激动剂，可用于腔内膀胱癌的研究。

BAY-9683 是一种口服有效的共价 PPARG 反向激动剂，可用于过度激活的 PPARG 疾病研究，如管腔膀胱癌。