ANQ 11125Motilin receptor antagonist,selective CAS# 153966-48-4 |
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Quality Control & MSDS
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Chemical structure
3D structure
| Cas No. | 153966-48-4 | SDF | Download SDF |
| PubChem ID | 90489005 | Appearance | Powder |
| Formula | C86H125N19O21 | M.Wt | 1761.05 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc. | ||
| Sequence | FVFIFTYGELQRLQ | ||
| SMILES | CCC(C)C(C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)O)C(=O)NC(CC2=CC=C(C=C2)O)C(=O)NCC(=O)NC(CCC(=O)O)C(=O)NC(CC(C)C)C(=O)NC(CCC(=O)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC(C)C)C(=O)NC(CCC(=O)N)C(=O)O)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(C(C)C)NC(=O)C(CC4=CC=CC=C4)N | ||
| Standard InChIKey | YQKDYBMNXFOSLF-SDGXXZENSA-N | ||
| Standard InChI | InChI=1S/C86H125N19O21/c1-10-49(8)71(104-80(120)64(42-52-23-16-12-17-24-52)101-82(122)70(48(6)7)103-73(113)56(87)41-51-21-14-11-15-22-51)83(123)102-65(43-53-25-18-13-19-26-53)81(121)105-72(50(9)106)84(124)100-63(44-54-28-30-55(107)31-29-54)74(114)93-45-68(110)94-58(34-37-69(111)112)76(116)99-61(39-46(2)3)78(118)96-59(32-35-66(88)108)77(117)95-57(27-20-38-92-86(90)91)75(115)98-62(40-47(4)5)79(119)97-60(85(125)126)33-36-67(89)109/h11-19,21-26,28-31,46-50,56-65,70-72,106-107H,10,20,27,32-45,87H2,1-9H3,(H2,88,108)(H2,89,109)(H,93,114)(H,94,110)(H,95,117)(H,96,118)(H,97,119)(H,98,115)(H,99,116)(H,100,124)(H,101,122)(H,102,123)(H,103,113)(H,104,120)(H,105,121)(H,111,112)(H,125,126)(H4,90,91,92)/t49-,50+,56-,57-,58-,59-,60-,61-,62-,63-,64-,65-,70-,71-,72-/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 | Selective motilin receptor antagonist (pKd = 8.24). Exhibits no effect on acetylcholine, substance P or serotonin stimulated intestinal contraction. |
ANQ 11125 Dilution Calculator
ANQ 11125 Molarity Calculator
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ANQ 11125 is a selective antagonist of motilin receptor with pKd of 8.24 [1].
Motilin receptor is a G protein-coupled receptor for motilin and stimulates contraction of gut smooth muscle.
ANQ 11125 is a selective motilin receptor antagonist. The affinity of ANQ 11125 for motilin receptor is about 10 times less than motilin [1]. In rabbit antral smooth muscle tissue, ANQ-11125 bound to motilin receptor with pKd value of 8.16. While, ANQ-11125 didn’t induce contractions of rabbit duodenum. ANQ-11125 (10-5 M) induced contractile response by 29% compared to ACh [2].
References:
[1]. Depoortere I, Macielag MJ, Galdes A, et al. Antagonistic properties of [Phe3,Leu13]porcine motilin. Eur J Pharmacol, 1995, 286(3): 241-247.
[2]. Peeters TL, Depoortere I, Macielag MJ, et al. The motilin antagonist ANQ-11125 blocks motilide-induced contractions in vitro in the rabbit. Biochem Biophys Res Commun, 1994, 198(2): 411-416.
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The motilin antagonist ANQ-11125 blocks motilide-induced contractions in vitro in the rabbit.[Pubmed:8297350]
Biochem Biophys Res Commun. 1994 Jan 28;198(2):411-6.
Studies on the physiological role of motilin, and more recently, on the relationship between motilin and erythromycin A, have been hampered by the lack of antagonists. We now have discovered such a compound. ANQ-11125 displaces motilin bound to an homogenate of rabbit antral smooth muscle tissue. The dissociation constant (pKd) was 8.16 +/- 0.10. However, ANQ-11125 did not induce contractions of segments of rabbit duodenum, except at high concentrations. In the presence of 1 microM ANQ-11125 the dose response curves of erythromycin-A, De(N-methyl)-N-ethyl-8,9 anhydroerythromycin A 6,9-hemiacetal and motilin were shifted about one log unit to the right, but the responses to ACh and Substance P were unaffected. Schild-analysis showed the competitive nature of the interaction and allowed the calculation of the pA2: 7.03 +/- 0.05 (motilin curves) and 7.55 +/- 0.06 (EM-523 curves). This is the first report of a motilin antagonist. Its properties definitively prove that motilides are motilin agonists.
Antagonistic properties of [Phe3,Leu13]porcine motilin.[Pubmed:8608785]
Eur J Pharmacol. 1995 Nov 24;286(3):241-7.
We describe the antagonistic properties due to the replacement of Pro3 by phenylalanine in porcine motilin. The analogue, [Phe3,Leu13] porcine motilin (OHM-11526), displaces iodinated [Nle13]porcine motilin bound to a homogenate of rabbit antral smooth muscle tissue. The dissociation constant (pKd) was 9.26 +/- 0.04, versus 9.11 +/- 0.01 for motilin and 8.24 +/- 0.06 for ANQ-11125, the (1-14) fragment of OHM-11526. The Hill coefficient was close to one and Schild plot analysis confirmed the competitive nature of the interaction. In the tissue bath OHM-11526 was unable to induce contractions of segments of rabbit duodenum. At a concentration of 10(-6) M, OHM-11526 was unable to induce contractions of segments of rabbit duodenum. At a concentration of 10(-6) M, OHM-11526 inhibited the effect of maximally effective doses of porcine motilin and of the erythromycin derivative, EM-523, but was without effect on contractions induced by acetylcholine, substance P and serotonin. Increasing doses of OHM-11526 shifted the dose-response curves of motilin and EM-523 to the right, but caused a depression of the maximal response as well. From the motilin curves, and assuming a dual competitive and non-competitive interaction, the pA2 was 7.79 +/- 0.08, the pD'2 6.91 +/- 0.08. The EM-523 curves yielded comparable data (pA2 = 8.10 +/- 0.12 and pD'2 = 7.06 +/- 0.13). OHM-11526 also blocked the motilin responses observed with smooth muscle strips from the rabbit and human antrum. However, in a preparation of the chicken small intestine, OHM-11526 was a full agonist with a potency (pD2 = 6.84) comparable to that of porcine motilin (pD2 = 6.71). Our data confirm the interaction of motilides with the motilin receptor. Due to its increased affinity for the motilin receptor, OHM-11526 will be a valuable took for studying the physiology of motilin and the pharmacology of motilin and motilides.
