| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
CCK-B receptor (cholecystokinin B/gastrin receptor) [4]
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|---|---|
| ln Vitro |
In receptor autoradiography, (Leu15)-Gastrin I (human) labeled with iodine-125 showed high-density specific binding to CCK-B receptors in the midglandular region of human gastric fundic mucosa, correlating with parietal cell distribution. Binding was displaceable by unlabeled gastrin and sulfated CCK-8. No binding was detected in human antral mucosa. A low density of CCK-B receptors was also identified in the circular muscle layer of the fundus [4].
In rat gastric fundus, (Leu15)-Gastrin I (human) labeled the whole mucosa with lower intensity in the midglandular region [4]. |
| Enzyme Assay |
Receptor autoradiography procedure for CCK-B/gastrin receptors using (Leu15)-Gastrin I (human): Cryostat sections (10-20 μm) of human gastric tissues were preincubated in 50 mmol/L Tris-HCl (pH 7.4) with 130 mmol/L NaCl, 4.7 mmol/L KCl, 5 mmol/L MgCl, 1 mmol/L EGTA, and 0.5% bovine serum albumin for 30 min at 25°C. Sections were then incubated with 55 pmol/L (Leu15)-Gastrin I (human) labeled with iodine-125 (2000 Ci/mmol) in the same buffer without bovine serum albumin, supplemented with 0.025% bacitracin, 1 mmol/L dithiothreitol, 2 μg/mL chymostatin, and 4 μg/mL leupeptin (pH 6.5) for 150 min at room temperature. Non-specific binding was determined with 100 nmol/L unlabeled gastrin. After incubation, slides were washed 6×15 min in ice-cold preincubation buffer (pH 7.4), rinsed twice in ice-cold distilled water, dried under cold air, and exposed to Hyperfilm for 1-7 days. Autoradiograms were quantified using computer-assisted image processing with iodinated tissue standards [4].
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| References | |
| Additional Infomation |
(Leu15)-Gastrin I (human) (also called Leu15-little gastrin or HG 17) was synthesized by solid-phase methods using 2-chlorotrityl resin and Fmoc/tBu strategy. The protected form (4b) was cleaved from resin with acetic acid/trifluoroethanol/dichloromethane (1:2:7 or 2:2:6) for 30 min at room temperature, giving 99% yield and >95% purity by HPLC. Full deprotection with TFA/water (95:5) or TFA/anisole (7:3) yielded free peptide (4c) in 63-64% after HPLC purification; structure confirmed by FAB-MS (m/z 2081 for MH+) [3]. In another study, crude protected (Leu15)-Gastrin I (human) (15a) was obtained in 99% yield using 2-chlorotrityl chloride resin, and free peptide (16) in 92% yield with 90% purity [1]. The compound was used as a radioligand for CCK receptor mapping in human stomach [4].
|
| Molecular Formula |
C98H126N20O31
|
|---|---|
| Molecular Weight |
2080.16000
|
| Exact Mass |
2078.89
|
| CAS # |
39024-57-2
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| PubChem CID |
16170068
|
| Appearance |
White to off-white solid powder
|
| LogP |
3.656
|
| Hydrogen Bond Donor Count |
26
|
| Hydrogen Bond Acceptor Count |
31
|
| Rotatable Bond Count |
61
|
| Heavy Atom Count |
149
|
| Complexity |
4740
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| Defined Atom Stereocenter Count |
15
|
| SMILES |
C[C@@H](C(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)NCC(=O)N[C@@H](CC2=CNC3=CC=CC=C32)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC4=CC=CC=C4)C(=O)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC5=CNC6=CC=CC=C65)NC(=O)[C@@H]7CCCN7C(=O)CNC(=O)[C@@H]8CCC(=O)N8
|
| InChi Key |
CMVMLPDUAGUTOC-FPBFVHJESA-N
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| InChi Code |
InChI=1S/C98H126N20O31/c1-49(2)38-68(115-96(147)72(43-55-46-101-60-19-12-10-17-58(55)60)117-98(149)74-20-13-37-118(74)77(122)48-103-86(137)61-25-31-75(120)105-61)93(144)111-66(30-36-82(131)132)92(143)110-65(29-35-81(129)130)91(142)109-64(28-34-80(127)128)90(141)108-63(27-33-79(125)126)89(140)107-62(26-32-78(123)124)88(139)104-51(5)85(136)113-70(41-53-21-23-56(119)24-22-53)87(138)102-47-76(121)106-71(42-54-45-100-59-18-11-9-16-57(54)59)95(146)114-69(39-50(3)4)94(145)116-73(44-83(133)134)97(148)112-67(84(99)135)40-52-14-7-6-8-15-52/h6-12,14-19,21-24,45-46,49-51,61-74,100-101,119H,13,20,25-44,47-48H2,1-5H3,(H2,99,135)(H,102,138)(H,103,137)(H,104,139)(H,105,120)(H,106,121)(H,107,140)(H,108,141)(H,109,142)(H,110,143)(H,111,144)(H,112,148)(H,113,136)(H,114,146)(H,115,147)(H,116,145)(H,117,149)(H,123,124)(H,125,126)(H,127,128)(H,129,130)(H,131,132)(H,133,134)/t51-,61-,62-,63-,64-,65-,66-,67-,68-,69-,70-,71-,72-,73-,74-/m0/s1
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| Chemical Name |
(4S)-5-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-[[(2S)-4-carboxy-2-[[(2S)-4-carboxy-2-[[(2S)-4-carboxy-2-[[(2S)-4-carboxy-2-[[(2S)-2-[[(2S)-3-(1H-indol-3-yl)-2-[[(2S)-1-[2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]butanoyl]amino]butanoyl]amino]butanoyl]amino]butanoyl]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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~10.53 mg/mL (~5.06 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 | 0.4807 mL | 2.4037 mL | 4.8073 mL | |
| 5 mM | 0.0961 mL | 0.4807 mL | 0.9615 mL | |
| 10 mM | 0.0481 mL | 0.2404 mL | 0.4807 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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