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| 5mg |
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| Targets |
Motilin, canine primarily targets the Motilin Receptor (MLN-R), which is a G protein-coupled receptor (GPCR). The MLN-R is found in various mammals and has also been identified in non-mammalian vertebrates. The receptor is expressed in the smooth muscle and enteric nervous system of the gut. Binding of motilin to its receptor activates cholinergic signaling that induces contractions in intestinal muscle. In preadipocytes, motilin increases metabolic activity. The compound's biological activity is mediated through specific GPCR signaling pathways in gastrointestinal tissues.
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| ln Vitro |
In vitro studies have characterized canine motilin as a potent agonist for gastrointestinal smooth muscle contraction. The peptide induces dose-dependent contractions in canine duodenal tissue with an EC50 of 4.82×10-⁵ M, where porcine motilin is inactive, demonstrating species specificity. It has been validated as a radioligand for motilin receptor binding studies with a Kd of 0.9+/-0.6 nM on human antral smooth muscle and a Bmax of 77+/-9 fmol/mg protein. The compound's activity is mediated through the specific motilin receptor MLN-R.
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| ln Vivo |
Motilin has been suggested to control the onset of phase III of the migratory motor complex (MMC) in humans and dogs. It is a strong agonist of smooth muscle contraction in the gastrointestinal tract. In addition to inducing pancreatic secretion, motilin also contracts the gallbladder and the sphincter of Oddi in dogs but not in humans. In canine jejunal round smooth muscle cells, motilin activates L-type Ca2+ channels (IcaL) via a G protein-coupled mechanism. In canine jejunal round smooth muscle cells, motilin at 1 μM can raise IcaL by 43±20[1].
In vivo studies demonstrate that motilin mediates the phase III of interdigestive migrating motor complex (MMC) in the stomach of humans, dogs, and house musk shrews through the specific motilin receptor (MLN-R). The peptide is released during fasting and regulates gastrointestinal motility. Canine motilin induces contractions in intestinal muscle by binding the motilin receptor and activating cholinergic signaling. The peptide controls the onset of phase III of the MMC. Species-specific differences in motilin activity have been observed, with canine motilin showing distinct activity compared to porcine motilin. |
| Enzyme Assay |
The in vitro enzyme/receptor binding assay for motilin, canine typically involves radioligand binding studies using membrane preparations from tissues expressing the motilin receptor (MLN-R). Competitive binding assays are performed with varying concentrations of unlabeled motilin and a radiolabeled motilin ligand to determine binding affinity (Kd). The assay has been validated with a Kd of 0.9+/-0.6 nM on human antral smooth muscle. Scatchard analysis is used to determine receptor density (Bmax). Data analysis using nonlinear regression models yields binding parameters. The specificity of binding is confirmed using related peptides.
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| Cell Assay |
In vitro cellular assays for motilin, canine are conducted using cells expressing the motilin receptor, such as smooth muscle cells or transfected cell lines. Cells are treated with varying concentrations of canine motilin, and receptor activation is assessed by measuring downstream signaling, such as calcium mobilization or cAMP modulation. Functional activity is evaluated by measuring smooth muscle contraction in isolated tissue preparations. The EC50 for contraction in canine duodenal tissue is 4.82×10-⁵ M. Cell viability and specificity are confirmed using appropriate controls and receptor antagonists.
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| Animal Protocol |
In vivo animal studies for motilin, canine are typically performed in dogs or other mammals to evaluate gastrointestinal motility. The peptide is administered intravenously or intra-arterially, and gastrointestinal contractile activity is measured using manometry or strain gauge transducers. The migrating motor complex (MMC) is monitored during fasting and postprandial states. Dose-response relationships are established for motilin-induced contractions. Studies may also evaluate the effects of motilin receptor antagonists to confirm receptor-mediated effects. Blood samples are collected for pharmacokinetic analysis of the peptide.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for motilin, canine are limited as it is a peptide hormone used primarily for research purposes. As a 22-amino acid peptide with a molecular weight of approximately 2685 Da, motilin is susceptible to rapid degradation by proteases in the gastrointestinal tract and bloodstream. The peptide has a short half-life in circulation. When administered systemically, it is rapidly cleared. For in vivo studies, the peptide is typically administered via injection rather than oral routes due to poor oral bioavailability. Its distribution is primarily to gastrointestinal tissues where the motilin receptor is expressed.
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| Toxicity/Toxicokinetics |
Toxicology data for motilin, canine are not extensively reported, as the peptide is a naturally occurring hormone used for research applications. As a 22-amino acid peptide, it is expected to have low immunogenicity in canine species. Standard toxicity assessments for peptide research compounds would include evaluation of acute toxicity, local tolerance at injection sites, and potential immunogenic responses. No specific toxicity data, including LD50 values or organ toxicity profiles, are readily available in the public domain. The peptide is for research use only and not for human therapeutic applications.
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| References | |
| Additional Infomation |
Motilin, canine is a 22-amino acid peptide hormone (sequence: FVPIFTHSELQKIREKERNKGQ) originally purified from canine small intestinal mucosa. It is a potent agonist of gastrointestinal smooth muscle contraction and mediates the phase III of interdigestive migrating motor complex through the specific motilin receptor (MLN-R). The peptide is used as a research tool for studying gastrointestinal motility. It is available as a lyophilized powder for research applications. Canine motilin shows species specificity, with porcine motilin being inactive in canine tissues.
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| Molecular Formula |
C120H194N36O34
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|---|---|
| Molecular Weight |
2685.04516
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| Exact Mass |
2683.46
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| CAS # |
85490-53-5
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| PubChem CID |
71311666
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| Appearance |
White to off-white solid powder
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| LogP |
4.289
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| Hydrogen Bond Donor Count |
40
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| Hydrogen Bond Acceptor Count |
41
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| Rotatable Bond Count |
96
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| Heavy Atom Count |
190
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| Complexity |
5950
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| Defined Atom Stereocenter Count |
24
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| SMILES |
CC[C@H](C)[C@@H](C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC2=CNC=N2)C(=O)N[C@@H](CO)C(=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](CCCCN)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCCNC(=N)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
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| InChi Key |
UXNMKJPZQNQTMI-CSRYRKIZSA-N
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| InChi Code |
InChI=1S/C120H194N36O34/c1-10-64(7)95(114(185)146-75(35-25-51-134-120(130)131)101(172)143-77(39-44-91(163)164)104(175)139-72(32-19-22-48-122)100(171)142-78(40-45-92(165)166)105(176)141-74(34-24-50-133-119(128)129)102(173)148-84(57-89(127)161)110(181)138-71(31-18-21-47-121)99(170)135-59-90(162)137-80(118(189)190)38-43-88(126)160)153-107(178)73(33-20-23-49-123)140-103(174)76(37-42-87(125)159)144-108(179)81(53-62(3)4)147-106(177)79(41-46-93(167)168)145-112(183)85(60-157)151-109(180)83(56-69-58-132-61-136-69)150-116(187)97(66(9)158)155-111(182)82(55-68-29-16-13-17-30-68)149-115(186)96(65(8)11-2)154-113(184)86-36-26-52-156(86)117(188)94(63(5)6)152-98(169)70(124)54-67-27-14-12-15-28-67/h12-17,27-30,58,61-66,70-86,94-97,157-158H,10-11,18-26,31-57,59-60,121-124H2,1-9H3,(H2,125,159)(H2,126,160)(H2,127,161)(H,132,136)(H,135,170)(H,137,162)(H,138,181)(H,139,175)(H,140,174)(H,141,176)(H,142,171)(H,143,172)(H,144,179)(H,145,183)(H,146,185)(H,147,177)(H,148,173)(H,149,186)(H,150,187)(H,151,180)(H,152,169)(H,153,178)(H,154,184)(H,155,182)(H,163,164)(H,165,166)(H,167,168)(H,189,190)(H4,128,129,133)(H4,130,131,134)/t64-,65-,66+,70-,71-,72-,73-,74-,75-,76-,77-,78-,79-,80-,81-,82-,83-,84-,85-,86-,94-,95-,96-,97-/m0/s1
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| Chemical Name |
(2S)-5-amino-2-[[2-[[(2S)-6-amino-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-6-amino-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-amino-3-phenylpropanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-4-methylpentanoyl]amino]-5-oxopentanoyl]amino]hexanoyl]amino]-3-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]hexanoyl]amino]-4-carboxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-oxobutanoyl]amino]hexanoyl]amino]acetyl]amino]-5-oxopentanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~37.24 mM)
DMSO : ~20 mg/mL (~7.45 mM) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.3724 mL | 1.8622 mL | 3.7243 mL | |
| 5 mM | 0.0745 mL | 0.3724 mL | 0.7449 mL | |
| 10 mM | 0.0372 mL | 0.1862 mL | 0.3724 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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