Chemical Property of H-Phe-Val-Pro-xiIle-Phe-xiThr-Tyr-Gly-Glu-Leu-Gln-Arg-Met-Gln-Glu-Lys-Glu-Arg-Asn-Lys-Gly-Gln-OH
Chemical Property:
- PSA：1191.49000
- LogP:4.75460
- Storage Temp.:−20°C
- XLogP3:-14
- Hydrogen Bond Donor Count:39
- Hydrogen Bond Acceptor Count:41
- Rotatable Bond Count:95
- Exact Mass:2698.3730598
- Heavy Atom Count:190
- Complexity:6010
- Purity/Quality:
-
99%, *data from raw suppliers
Motilin *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
-
SDS file from LookChem
Total 1 MSDS from other Authors
Useful:
- Canonical 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(CCSC)C(=O)NC(CCC(=O)N)C(=O)NC(CCC(=O)O)C(=O)NC(CCCCN)C(=O)NC(CCC(=O)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC(=O)N)C(=O)NC(CCCCN)C(=O)NCC(=O)NC(CCC(=O)N)C(=O)O)NC(=O)C3CCCN3C(=O)C(C(C)C)NC(=O)C(CC4=CC=CC=C4)N
- Isomeric SMILES:CCC(C)[C@@H](C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](C(C)O)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCC(=O)N)C(=O)O)NC(=O)[C@@H]3CCCN3C(=O)[C@H](C(C)C)NC(=O)[C@H](CC4=CC=CC=C4)N
-
Biological functions
MLNR is mainly found in the GI tract, but the exact
localization is species-dependent. In humans, through
binding experiments with iodinated porcine [Leu13]
MLN, the MTLR density was found to be the highest in
the gastroduodenal region, and decreased distally in
the small intestine toward the colon. MLNR immunoreactivity is present in muscle cells and the myenteric
plexus, but not in mucosal or submucosal cells, in
humans. In rabbits, the highest MLNR density is found
in the colon. MLNR has been found outside the GI tract
in the hypothalamus, nodose ganglion, thyroid, and bone
marrow. Mlnr gene expression has been found in the
lung and heart in Suncus murinus, suggesting that MLN
could have an unknown function in the respiratory and
cardiovascular systems.The main biological functions are to increase lower esophageal sphincter (LES) pressure and to induce the interdigestive motor complex (IMC) for removing debris and
cleaning the GI tract. Recent studies in humans show that
MLN-induced gastric contractions stimulate hunger.
-
Description
Motilin was isolated from the duodenojejunal mucosa and
found to control the motor activity of the digestive tract. It is
a potential therapeutic drug target for improving digestive
dysmotility. Motilin was isolated from a side fraction produced
during the purification of secretin in 1971 and was
found to stimulate contractility in the fundus of the stomach. Complete porcine and human motilin were purified
and sequenced in 1973 and 1983 respectively.
-
Clinical Use
To date, almost all macrolides have lacked effectiveness as MLN agonists. However, pharmacies have been
trying to develop new types of macrolides, such as
PF-04548043 (formerly known as KOS-2187), for the treatment of GI motility disorders such as gastroparesis and
gastroesophageal reflux disease. Moreover, the new
MLNR agonist RQ-00201894 is a promising drug for
the treatment of gastroparesis, postoperative ileus, and
functional dyspepsia.
