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Search Results for " ileum "

43

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T11428	Glyco-Obeticholic acid	FXR	Metabolism
	Glyco-obeticholic acid 是一种牛磺酸的特性代谢物。Obeticholic Acid 是口服具有活性的法尼样 X 受体激动剂。
T14326	AS-35	Others	Others
	AS-35 is an orally effective, potent and selective antagonist of leukotrienes, antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum. With IC50 values of 8 nM, 4 nM and 3 nM, respectively. It has antiallergic activities.
TP1819L	Substance P 1-9 aceate	Neurotensin Receptor	GPCR/G Protein
	Substance P 1-9 aceate 是九肽，可减少豚鼠回肠和膀胱对 P 物质的失活。
T12756	ROS 234 dioxalate	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	ROS 234 dioxalate is a potent antagonist of H3(pKB of 9.46 for Guinea-pig ileum H3-receptor)
T33449	ML 1035 ML103,ML-1035
	ML 1035 is a benzamide that elicits contractions from guinea-pig non-stimulated ileum.
T27140	Delequamine HCl RS-15385,RS15385,RS 15385,Delequamine,RS-15385-197
	Delequamine HCl is a potent and selective alpha 2-adrenoceptor antagonist. Delequamine HCl has a pKi of 9.45 for alpha 2-adrenoceptors in the rat cortex (pA2 in the guinea-pig ileum of 9.72).
T8437	3-(4-prop-2-en-1-ylpiperazin-1-yl)quinox	Others	Others
	3-(4-prop-2-en-1-ylpiperazin-1-yl)quinox 拮抗 2-methyl-5-HT 诱导的豚鼠回肠收缩。
T23829	Btm 1042 Btm1042,Btm-1042
	Btm 1042 is an antispasmodic drug. It has been found to depress twitch responses in the ileum of guinea pigs.
T37494	11-trans Leukotriene E4 11-trans Leukotriene E4
	Slow isomerization of the C-11 double bond of LTE4 leads to the formation of 11-trans LTE4. 11-trans LTE4 is equipotent to LTE4 in contracting guinea pig ileum.
TP1171	Apraglutide TFA (1295353-98-8 free base) Apraglutide TFA,FE 203799e (TFA)
	Apraglutide TFA (FE 203799 TFA), a synthetic 33-amino-acid peptide and a long-acting GLP-2 analogue, enhances adaptation and linear intestinal growth in a neonatal piglet model of short bowel syndrome with total resection of the ileum.
TP2012	JMV 449
	Potent, metabolically stable neurotensin receptor agonist peptide (IC50 = 0.15 nM for inhibition of [125I]-NT binding to neonatal mouse brain; EC50 = 1.9 nM for contraction of guinea pig ileum). Produces long-lasting hypothermic, neuroprotective and analg
T70688	S 0960
	S 0960 is a dimeric bile acid analogue that acts as a specific inhibitor of the apical sodium-dependent bile salt transporter (ASBT) in the ileum.
TP1819	Substance P (1-9)
	Substance P (1-9) is nonapeptide, which decreases the inactivation of substance P by the guinea-pig ileum and urinary bladder. Subtance P is responsible for a number of excitatory effects on both central and peripheral neurons.
TP1988	[Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2
	Potent agonist of the nociceptin (ORL1) receptor, demonstrated both in vitro and in vivo. Selective, competitive antagonism at the nociceptin receptor has also been reported (pA2 = 7.02 and 6.75 in the guinea pig ileum and mouse vas deferens respectively)
T78563	[Leu13]-Motilin KW-5139	Motilin Receptor	GPCR/G Protein
	[Leu13]-Motilin (KW-5139) 为motilin类似物，能够刺激家兔胃肠运动，并在体外以浓度依赖性方式引起胃窦、十二指肠、空肠、回肠以及降结肠的收缩。
T69126	Clofeverine (free base)
	Clofeverine (free base) is a highly selective relaxant for gastrointestinal smooth muscles with a beta-receptor stimulative nature. On isolated ileum, the inhibitory effect of clofeverine for spontaneous motility was comparable to that of isoproterenol and 100 times higher than that of papaverine.
T71935	WIN 66306
	WIN 66306 is a cyclic heptapeptide antagonist of neurokinin-1 (NK1) and NK2 receptors originally isolated from A. flavipes. It binds to NK1 and NK2 receptors and inhibits contractions induced by substance P in isolated guinea pig ileum in a concentration-dependent manner.
T37652	5(S),6(R)-DiHETE
	5(S),6(R)-DiHETE is a dihydroxy polyunsaturated fatty acid and a nonenzymatic hydrolysis product of leukotriene A4 (LTA4). Mouse liver cytosolic epoxide hydrolase catalyzes the conversion of LTA4 to 5(S),6(R)-DiHETE. It is a weak LTD4 receptor agonist in guinea pig lung membranes. It induces guinea pig ileum contraction with an ED50 value of 1.3 μM.
T37492	11-trans Leukotriene C4 11-trans Leukotriene C4
	11-trans Leukotriene C4 (11-trans LTC4) is a C-11 double bond isomer of LTC4. LTC4 undergoes slow temperature-dependent isomerization to 11-trans LTC4 during storage. 11-trans LTC4 is produced in smaller amounts relative to LTC4 in ionophore-stimulated HMC-1 cells (a human mast cell line) and equine eosinophils, but not in human neutrophils or RBL-1 cells. It is nearly equipotent with LTC4 for contraction of guinea pig parenchymal and ileum. In a radioligand binding assay using guinea pig ileum ...
T37493	11-trans Leukotriene D4 11-trans Leukotriene D4
	11-trans Leukotriene D4 (11-trans LTD4) is a C-11 double bond isomer of LTD4. LTD4 undergoes slow temperature-dependent isomerization to 11-trans LTD4 during storage. 11-trans LTD4 retains about 10-25 % of the potency for contraction of guinea pig ileum, trachea and parenchyma compared to LTD4. It exhibits an ED50 ranging between 12-60 nM for contraction of guinea pig trachea.
TP2075	Bombinakinin M
	Potent bradykinin receptor agonist. Highly selective for mammalian arterial smooth muscle bradykinin receptors, displaying ~ 50-fold greater potency than bradykinin. Elicits dose-dependent contractile effects in smooth muscle of guinea pig ileum (EC50 = 4
T69324	Clofeverine hydrochloride
	Clofeverine hydrochloride is the salt form of Clofeverine (free base), a highly selective relaxant for gastrointestinal smooth muscles with a beta-receptor stimulative nature. On isolated ileum, the inhibitory effect of clofeverine for spontaneous motility was comparable to that of isoproterenol and 100 times higher than that of papaverine.
T81079	Substance P (2-11)
	Substance P (2-11)为P物质（SP）片段肽，具有对豚鼠回肠产生收缩活性的特性。同时，Substance P (2-11)能够抑制3H SP在BBMEC单分子层中的渗透。
T83497	[D-Pro2,D-Phe7,D-Trp9] Substance P
	[D-Pro2,D-Phe7,D-Trp9]Substance P为Substance P的模拟物，并充当其抑制剂，能间接收缩豚鼠回肠。
T81078	Substance P (3-11)
	Substance P (3-11)，作为P 物质 (SP) 的片段肽，具备穿透血脑屏障的能力，且对豚鼠回肠显示出收缩活性。
T76001	Apraglutide TFA
	Apraglutide TFA (FE 203799 TFA) 是一种合成的、含33个氨基酸的肽类药物，为长效GLP-2类似物。它能在全回肠切除后导致的新生短肠综合征小猪中增强适应性和线性肠生长。
T60340	ROS 234
	ROS 234 is a highly effective H3 antagonist, demonstrating a strong binding affinity (pK B) of 9.46 for the Guinea-pig ileum H3 receptor and a pKi of 8.90 for the Rat cerebral cortex H3 receptor. Additionally, it exhibits an ex vivo ED50 of 19.12 mg/kg (ip) in the Rat cerebral cortex. It should be noted that ROS 234 demonstrates limited central access, as reported in [1] and [2].
T26770	Bencycloquidium Bromide BCQB
	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
T37206	CCK (27-33) (non-sulfated)
	CCK (27-33) is a C-terminal fragment of CCK , a peptide hormone found in the intestine and brain that stimulates digestion, mediates satiety, and is involved in anxiety. Non-sulfated CCK (27-33) inhibits binding of [3H]naloxone in rat cerebellum membranes (IC50 = 4 uM) and inhibits electrically-stimulated contraction of isolated guinea pig ileum (IC50 = 17 uM), an effect that can be reversed by naloxone. Unlike sulfated CCK (27-33), the non-sulfated form does not reduce exploratory behavior in m...
T70267	ADL 08-0011 HCl
	ADL 08-0011 is an active metabolite of the μ-opioid receptor antagonist alvimopan. It is produced from alvimopan via amide hydrolysis by gut microbiota. ADL 08-0011 is a μ-opioid receptor antagonist (Ki = 0.25 nM). It is selective for μ-opioid receptors over κ- and δ-opioid receptors (Kis = 15.8 and 31.6 nM, respectively). ADL 08-0011 inhibits endomorphin 1-induced inhibition of electrically induced contraction of isolated guinea pig ileum (pA2 = 9.4). In vivo, ADL 08-0011 (0.03-1 mg/kg) reverse...
T10294	AM9405	5-HT Receptor	GPCR/G Protein; Neuroscience
	AM9405是一种新型的外周活性大麻素1型 (CB1)和5-羟色胺3型受体激动剂。 AM9405抑制回肠和结肠的抽搐收缩，IC50分别为45.71 和 0.076 nM。AM9405 在生理条件下显着减缓小鼠肠道蠕动.
T37996	17-phenyl trinor Prostaglandin E2 ethyl amide 17-phenyl trinor Prostaglandin E2 ethyl amide
	17-phenyl trinor PGE2 ethyl amide is derived from 17-phenyl trinor PGE2, a synthetic analog of PGE2 that acts as an agonist of EP1 and EP3 receptors in mice (Ki = 14 and 3.7 nM, respectively) and EP1, EP3, and EP4 in rats (Ki = 25, 4.3, and 54 nM, respectively). 17-phenyl trinor PGE2 causes contraction of guinea pig ileum at a concentration of 11 μM and is 4.4 times more potent than PGE2 as an antifertility agent in hamsters. Modification of the C-1 carboxyl group to an ethyl amide serves to inc...
T39176	PB28
	PB28 is a cyclohexylpiperazine derivative that functions as a potent and highly selective agonist of the sigma 2 (σ2) receptor, exhibiting a Ki (binding affinity) of 0.68 nM. At the same time, PB28 acts as an antagonist of the sigma 1 (σ1) receptor, with a Ki of 0.38 nM. PB28 demonstrates a lower affinity for other receptors. It effectively inhibits electrically evoked twitch in both the guinea pig bladder (EC50 value of 2.62 μM) and ileum (EC50 value of 3.96 μM). Moreover, PB28 exhibits the abi...
T75868	JMV 449 acetate
	JMV 449 acetate 是一种有效的神经降压素受体 (neurotensin receptor) 激动剂。JMV 449 acetate 显示抑制125I-neurotensin 与新生小鼠脑结合的 IC50为 0.15 nM，对收缩豚鼠回肠的 EC50为 1.9 nM。JMV 449 acetate 对小鼠具有高效、持久的降温和缓解疼痛作用。
T73930	(-)-Eseroline fumarate
	(-)-Eseroline fumarate 是一种 AChE 抑制剂 Physostigmine 的代谢产物。(-)-Eseroline fumarate 引起癌细胞的乳酸脱氢酶 (LDH) 泄漏。(-)-Eseroline fumarate 还诱导神经元细胞释放腺嘌呤核苷酸和5-羟色胺 (5-HT)，从而诱导细胞死亡。(-)-Eseroline fumarate 抑制小鼠输精管和豚鼠回肠的电诱发抽搐。
T68219	Peraclopone
	Peraclopone is a hypolidemic drug. It is an inhibitor of 7-Dehydrocholesterol reductase. Peraclopone potently inhibits the final step in cholesterol biosynthesis. Feeding this agent to rats leads to a rapid replacement of membrane cholesterol with its immediate precursor 7-dehydrocholesterol, and a dramatic reduction in plasma sterol concentration. Peraclopone caused a dose-dependent decrease in cholesterol and a concomitant accumulation of provitamin D3 (7-dehydrocholesterol) in the skin, which...
T37261	14,15-Leukotriene D4 14,15-Leukotriene D4
	14,15-Leukotriene D4 (14,15-LTD4) is a member of an alternate class of LTs synthesized by a pathway involving the dual actions of 15- and 12-lipoxygenases (15- and 12-LOs) on arachidonic acid via 15-HpETE and 14,15-LTA4 intermediates. 14,15-LTD4 is classified as an eoxin (EXD4), because it is formed mostly by eosinophils. However, mast cells and nasal polyps can synthesize 14,15-LTD4 as well. Little is known about the physiological actions of 14,15-LTD4. It has weak contractile activity on both ...
T36554	TMB 8 (hydrochloride)
	TMB 8 is a non-competitive antagonist of nicotinic acetylcholine receptors (nAChRs) with IC50 values of 390 and 350 nM, respectively, for human muscle-type and α3β4 subunit-containing ganglionic nAChRs expressed in TE671/RD or SH-SY5Y cells. It inhibits nicotine-induced dopamine release from rat brain synaptosomes (IC50 = 480 nM). TMB 8 also reduces calcium availability in smooth and skeletal muscle, blocking the contractile response in isolated rabbit aortic strip when used at a concentration o...
T70456	Nolpitantium Free Base
	Nolpitantium Free Base is a highly selective nonpeptide antagonist of neurokinin-1 (NK1) receptor. Nolpitantium potently, selectively and competitively inhibited substance P binding to NK1 receptors from various animal species, including humans. In vitro, it was a potent antagonist in functional assays for NK1 receptors such as [Sar9, Met(O2)11]substance P-induced endothelium-dependent relaxation of rabbit pulmonary artery and contraction of guinea-pig ileum. Up to 1 mkM, Nolpitantium had no eff...
T36660	Olsalazine-13C6 Olsalazine-13C6
	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 ...
T12738	Rivanicline hemioxalate RJR-2403 hemioxalate,(E)-Metanicotine hemioxalate	Others	Others
	Rivanicline hemioxalate (RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate) 是一种神经元烟碱受体 (neuronal nicotinic receptor) 激动剂，对 α4β2 亚型有高度选择性(Ki= 26 nM)，比对于 α7 受体的选择性高1000倍(Ki=3.6 μM)。
T83768	Zofenoprilat Zofenopril-SH,SQ 26,333
	Zofenoprilat是一种血管紧张素转换酶(ACE; IC50 = 8 nM for the rabbit lung enzyme)的抑制剂，同时也是前体药zofenopril的活性代谢产物。它能够抑制分离的豚鼠小肠中由血管紧张素I或缓激肽诱导的收缩(EC50s = 3 and 1 nM, respectively)。在人类脐静脉内皮细胞(HUVECs)中，Zofenoprilat (10 nM)降低基础内皮素-1分泌和一氧化氮(NO)生成，并阻止TNF-α诱导的活性氧种(ROS)增加以及谷胱甘肽(GSH)水平降低。Zofenoprilat (10 µM)保护初级人类心脏微血管内皮细胞免受多柔比星诱导的细胞毒性。此外，Zofenoprilat (10 µM)还能增加HUVECs中的硫化氢(H2S)生成，以及细胞的黏着、迁移和增殖。在以400 µM浓度使用时，它可以减少Langendorff分离的大鼠心脏灌流缺血再灌注损伤模型中的舒张末压和乳酸脱氢酶(LDH)释放。
T36618	Rupatadine
	Rupatadine (UR-12592) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig cerebellum membranes).IC50 value:Target: PAF/H1 antagonistin vitro: Rupatadine competitively inhibited histamine-induced guinea pig ileum contraction (pA2 = 9.29 +/- 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). It also competitively inhibited PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2 = 6.68 +/- 0.08) and in hu...

化合物

Glyco-Obeticholic acid

Cat.No: T11428

Target: FXR

Cat.No: T14326

Target: Others

Substance P 1-9 aceate

Cat.No: TP1819L

Target: Neurotensin Receptor

ROS 234 dioxalate

Cat.No: T12756

Target: Histamine Receptor

Cat.No: T33449

Synonym: ML103,ML-1035

Delequamine HCl

Cat.No: T27140

Synonym: RS-15385,RS15385,RS 15385,Delequamine,RS-15385-197

3-(4-prop-2-en-1-ylpiperazin-1-yl)quinox

Cat.No: T8437

Target: Others

Cat.No: T23829

Synonym: Btm1042,Btm-1042

11-trans Leukotriene E4

Cat.No: T37494

Synonym: 11-trans Leukotriene E4

Apraglutide TFA (1295353-98-8 free base)

Cat.No: TP1171

Synonym: Apraglutide TFA,FE 203799e (TFA)

Cat.No: TP2012

Cat.No: T70688

Substance P (1-9)

Cat.No: TP1819

[Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2

Cat.No: TP1988

[Leu13]-Motilin

Cat.No: T78563

Synonym: KW-5139

Target: Motilin Receptor

Clofeverine (free base)

Cat.No: T69126

Cat.No: T71935

5(S),6(R)-DiHETE

Cat.No: T37652

11-trans Leukotriene C4

Cat.No: T37492

Synonym: 11-trans Leukotriene C4

11-trans Leukotriene D4

Cat.No: T37493

Synonym: 11-trans Leukotriene D4

Cat.No: TP2075

Clofeverine hydrochloride

Cat.No: T69324

Substance P (2-11)

Cat.No: T81079

[D-Pro2,D-Phe7,D-Trp9] Substance P

Cat.No: T83497

Substance P (3-11)

Cat.No: T81078

Apraglutide TFA

Cat.No: T76001

Cat.No: T60340

Bencycloquidium Bromide

Cat.No: T26770

Synonym: BCQB

CCK (27-33) (non-sulfated)

Cat.No: T37206

ADL 08-0011 HCl

Cat.No: T70267

Cat.No: T10294

Target: 5-HT Receptor

17-phenyl trinor Prostaglandin E2 ethyl amide

Cat.No: T37996

Synonym: 17-phenyl trinor Prostaglandin E2 ethyl amide

Cat.No: T39176

JMV 449 acetate

Cat.No: T75868

(-)-Eseroline fumarate

Cat.No: T73930

Cat.No: T68219

14,15-Leukotriene D4

Cat.No: T37261

Synonym: 14,15-Leukotriene D4

TMB 8 (hydrochloride)

Cat.No: T36554

Nolpitantium Free Base

Cat.No: T70456

Olsalazine-13C6

Cat.No: T36660

Synonym: Olsalazine-13C6

Rivanicline hemioxalate

Cat.No: T12738

Synonym: RJR-2403 hemioxalate,(E)-Metanicotine hemioxalate

Target: Others

Cat.No: T83768

Synonym: Zofenopril-SH,SQ 26,333

Cat.No: T36618

Cat. No.	Product Name	Target	Signaling Pathways
T13092	Tauro-Obeticholic acid	FXR	Metabolism
	Tauro-Obeticholic acid 是一种牛磺酸的特性代谢物。Obeticholic Acid 是口服具有活性的法尼样 X 受体激动剂。
T3A2467	Allocryptopine Thalictrimine,Fagarine I,别隐品碱	Potassium Channel	Membrane transporter/Ion channel
	Allocryptopine (Thalictrimine) 是一种延胡索乙素的衍生物，提取自Corydalis decumbens。Allocryptopine 具有抗心律失常作用，能有效阻断hERG 电流。
T3S2259	Methyl eugenol 4-allylveratrole,eugenyl methyl ether,O-methyleugenol,Eugenol Methyl ether,丁香酚甲醚,丁子香酚甲醚	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Methyl eugenol (4-allylveratrole) 是一种苯丙类化合物，存在于植物叶子、果实、根茎中，当植物相应的部位因食草动物进食而受损时，就会释放。它可用于消灭雄性东方果蝇。
TN4713	Onitisin	5-HT Receptor	GPCR/G Protein; Neuroscience
	Onitisin, onitinoside and onitin can inhibit the contraction of isolated guinea-pig ileum.
TN4812	Pluviatolide	AChR	Neuroscience
	(-)-Pluviatolide can inhibit electrically-induced and acetylcholine-induced contraction in the isolated guinea-pig ileum.

天然产物

Tauro-Obeticholic acid

Cat.No: T13092

Target: FXR

Cat.No: T3A2467

Synonym: Thalictrimine,Fagarine I,别隐品碱

Target: Potassium Channel

Cat.No: T3S2259

Synonym: 4-allylveratrole,eugenyl methyl ether,O-methyleugenol,Eugenol Methyl ether,丁香酚甲醚,丁子香酚甲醚

Target: GABA Receptor

Cat.No: TN4713

Target: 5-HT Receptor

Cat.No: TN4812

Target: AChR

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