IRL-1038ETB antagonist CAS# 144602-02-8 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 144602-02-8 | SDF | Download SDF |
| PubChem ID | 16130960 | Appearance | Powder |
| Formula | C68H92N14O15S2 | M.Wt | 1409.7 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 1 mg/ml in 20% acetonitrile | ||
| Sequence | CVYFCHLDIIW (Modifications: Disulfide bridge between 1 - 5) | ||
| Chemical Name | (3S)-3-[[(2S)-2-[[(2S)-2-[[(7S,13S,16R)-16-amino-7-benzyl-10-[(4-hydroxyphenyl)methyl]-6,9,12,15-tetraoxo-13-propan-2-yl-1,2-dithia-5,8,11,14-tetrazacycloheptadecane-4-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-[[(2S,3S)-1-[[(2S,3S)-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-oxobutanoic acid | ||
| SMILES | CCC(C)C(C(=O)NC(C(C)CC)C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)O)NC(=O)C(CC(=O)O)NC(=O)C(CC(C)C)NC(=O)C(CC3=CN=CN3)NC(=O)C4CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N4)CC5=CC=CC=C5)CC6=CC=C(C=C6)O)C(C)C)N | ||
| Standard InChIKey | OETKRDJJNWJFOP-PFAVPODXSA-N | ||
| Standard InChI | InChI=1S/C68H92N14O15S2/c1-9-37(7)56(66(94)78-52(68(96)97)27-41-30-71-46-19-15-14-18-44(41)46)82-67(95)57(38(8)10-2)81-63(91)51(29-54(84)85)76-59(87)47(24-35(3)4)73-62(90)50(28-42-31-70-34-72-42)75-64(92)53-33-99-98-32-45(69)58(86)80-55(36(5)6)65(93)77-49(26-40-20-22-43(83)23-21-40)60(88)74-48(61(89)79-53)25-39-16-12-11-13-17-39/h11-23,30-31,34-38,45,47-53,55-57,71,83H,9-10,24-29,32-33,69H2,1-8H3,(H,70,72)(H,73,90)(H,74,88)(H,75,92)(H,76,87)(H,77,93)(H,78,94)(H,79,89)(H,80,86)(H,81,91)(H,82,95)(H,84,85)(H,96,97)/t37-,38-,45-,47-,48-,49?,50-,51-,52-,53?,55-,56-,57-/m0/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | ETB endothelin receptor antagonist. |
IRL-1038 Dilution Calculator
IRL-1038 Molarity Calculator
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An endothelin B receptor-selective antagonist: IRL 1038, [Cys11-Cys15]-endothelin-1(11-21)[Pubmed:1397285]
FEBS Lett. 1992 Oct 12;311(1):12-6.
In the inhibition of specific binding of [125I]endothelins (ETs) to membrane from various tissues of rats, guinea pigs, pigs and humans, [Cys11-Cys15]-ET-1(11-21), IRL 1038, has a much higher affinity for ETB receptors (Ki = 6-11 nM) than for ETA receptors (Ki = 0.4-0.7 microM). In contraction assays, with ET-3 as a stimulant, 3 microM IRL 1038 antagonized the ETB receptor-mediated contraction of guinea pig ileal and tracheal smooth muscle without any significant agonistic activity, but did not effect the ETA receptor-mediated contraction of rat aortic smooth muscle. IRL 1038 is therefore, considered to be the first antagonist selective to the ETB receptor.
ETB receptor antagonist, IRL 1038, selectively inhibits the endothelin-induced endothelium-dependent vascular relaxation.[Pubmed:8449230]
Eur J Pharmacol. 1993 Feb 16;231(3):371-4.
In isolated rat aorta, endothelin-1 induced contractions at lower concentrations than endothelin-3. The contractile effects were augmented by removing the endothelium. In contrast, endothelium-1 and endothelin-3 at similar concentrations induced endothelium-dependent relaxation in norepinephrine-stimulated aorta. IRL 1038 ([Cys11,Cys15]endothelin-1(11-21); 3 microM) augmented the contractile effects of endothelins only in the presence of the endothelium. IRL 1038 (0.3-3 microM) inhibited the endothelium-dependent relaxation induced by endothelins but not by carbachol. IRL 1038 itself did not change muscle tension. These results suggest that IRL 1038 is a novel antagonist of the ETB receptor responsible for the release of relaxing factor from the vascular endothelium.
