オピオイド受容体
シグナル伝達経路
研究分野
- 阻害剤の選択性比較
- 溶解度
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S5701 | Alvimopan dihydrate (LY246736 dihydrate) | -1 mg/mL | 92 mg/mL | -1 mg/mL |
| S2503 | Racecadotril | <1 mg/mL | 22 mg/mL | 77 mg/mL |
| S3066 | Naloxone HCl | 72 mg/mL | 72 mg/mL | <1 mg/mL |
| S2722 | JTC-801 | <1 mg/mL | 90 mg/mL | 31 mg/mL |
| S2103 | Naltrexone HCl | 14 mg/mL | 14 mg/mL | <1 mg/mL |
| S2480 | Loperamide HCl | <1 mg/mL | 22 mg/mL | 4 mg/mL |
| S1139 | ADL5859 HCl | 5 mg/mL | 86 mg/mL | 1 mg/mL |
| S5087 | Tianeptine | -1 mg/mL | 87 mg/mL | -1 mg/mL |
| S2322 | (+)-Matrine | 11 mg/mL | 49 mg/mL | 49 mg/mL |
| S2085 | Trimebutine | <1 mg/mL | 50 mg/mL | <1 mg/mL |
| S4714 | (-)-Menthol | 16 mg/mL | 31 mg/mL | 31 mg/mL |
| S3204 | Meptazinol HCl | 53 mg/mL | 53 mg/mL | 53 mg/mL |
| S5701 | Alvimopan dihydrate (LY246736 dihydrate) | -1 mg/mL | 92 mg/mL | -1 mg/mL |
| S2503 | Racecadotril | <1 mg/mL | 22 mg/mL | 77 mg/mL |
| S4588 | Docusate Sodium | 18 mg/mL | 88 mg/mL | 88 mg/mL |
亜型選択性的な製品
- Opioid Receptor阻害剤(15)
- 新Opioid Receptor製品
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S5701新 |
Alvimopan dihydrate (LY246736 dihydrate)Alvimopan (LY-246736) is a potent, relatively nonselective opioid antagonist with Ki values of 0.77, 4.4, and 40 nM for the μ, δ, and κ opioid receptors, respectively, displaying >100-fold selectivity over other aminergic G-protein-coupled receptors. |
||
| S2503 |
RacecadotrilRacecadotril is a peripherally acting enkephalinase inhibitor with an IC50 of 4.5 μM. |
||
| S3066 |
Naloxone HClNaloxone HCl is an opioid inverse agonist drug used to counter the effects of opiate overdose. |
||
| S2722 |
JTC-801JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ. |
The effect of JTC-801 and naltrexone. (B) plasma IL-6 and (C) plasma TNF-α concentrations in the colon carcinoma model. The values represent the mean±SD derived from 6 animals. *, P<0.05
|
|
| S2103 |
Naltrexone HClNaltrexone HCl is an opioid receptor antagonist used primarily in the management of alcohol dependence and opioid dependence. |
(b) plasma IL-6 and (c) plasma tumornecrosis factor (TNF)-a concentrations in the colon carcinomamodel. The values represent the mean±SD derived from sixanimals. *P < 0.05
|
|
| S2480 |
Loperamide HClLoperamide HCl is a selective μ-opioid receptor agonist opioid with Ki of 3.3 nM, 15-fold and 350-fold selective over the δ subtype and the κ subtype of the opioid receptor, used against diarrhea resulting from gastroenteritis or inflammatory bowel disease. |
Low-micromolar amounts of loperamide inhibit MERS-CoV-induced cytopathology. Huh7 cells in 96-well plates were infected with MERS-CoV isolate EMC/2012 (MOI, 0.005) in the presence of 0 to 8 μM LPM (C). Cells were incubated for 2 days, and cell viability was monitored using an MTS assay. In addition, the potential toxicity of compound treatment only was monitored in parallel mock-infected Huh7 cell cultures. Graphs show the results (averages and standard deviations [SD]) of a representative experiment that was performed in quadruplicate. All experiments were repeated at least twice. For each compound, the calculated EC50, CC50, and SI values are given. |
|
| S1139 |
ADL5859 HClADL5859 HCl is a δ-opioid receptor agonist with Ki of 0.8 nM, selectivity against opioid receptor κ, μ, and weak inhibitory activity at the hERG channel. Phase 2. |
ADL-5859 respectively ADL-5747 were dopioid agonists (DORs) which were developed as analgesics for post-operative, neuropathic or musculoskeletal pain. They were expected to have superior analgesic potency over the existing ones, due to the different receptor targeted. However their development was stopped due to unconvincing efficacy. |
|
| S5087新 |
TianeptineTianeptine is an antidepressant agent that act as an atypical agonist of the μ-opioid receptor with clinically negligible effects on the δ- and κ-opioid receptors. |
||
| S2322 |
(+)-MatrineMatrine((+)-Matrine) is an alkaloid found in plants from the Sophora family, which has a variety of pharmacological effects, including anti-cancer effects, and action as a kappa opioid receptor agonist. |
||
| S2085 |
TrimebutineTrimebutine is an agonist of peripheral mu, kappa and delta opiate receptors, used as spasmolytic agent for treatment of both acute and chronic abdominal pain. |
||
| S4714 |
(-)-Menthol(-)-Menthol is a levo isomer of menthol and used as a cooling agent that strongly activates TRPM8. |
||
| S3204 |
Meptazinol HClMeptazinol is a unique centrally active opioid analgesic, which inhibits [3H]dihydromorphine binding with IC50 of 58 nM. |
||
| S5701新 |
Alvimopan dihydrate (LY246736 dihydrate)Alvimopan (LY-246736) is a potent, relatively nonselective opioid antagonist with Ki values of 0.77, 4.4, and 40 nM for the μ, δ, and κ opioid receptors, respectively, displaying >100-fold selectivity over other aminergic G-protein-coupled receptors. |
||
| S2503 |
RacecadotrilRacecadotril is a peripherally acting enkephalinase inhibitor with an IC50 of 4.5 μM. |
||
| S4588 |
Docusate SodiumDocusate Sodium is a laxative used to treat constipation, for constipation due to the use of opiates it maybe used with a stimulant laxative, can be taken by mouth or rectally. |
