| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 50mg | |||
| Other Sizes |
| Targets |
A 71623 selectively targets the cholecystokinin A (CCK-A) receptor, also known as the CCK1 receptor. CCK-A receptors are primarily located in the gastrointestinal tract and certain regions of the brain, including the area postrema and the nucleus tractus solitarius. They mediate the physiological effects of cholecystokinin (CCK), a peptide hormone that is released in response to food intake. Activation of CCK-A receptors on vagal afferent nerve endings sends satiety signals to the brain, leading to a reduction in food intake. A 71623 is a full agonist at this receptor, meaning it can elicit the maximum possible response.
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| ln Vitro |
A-71623 exhibits an affinity of 11 μM for the cholecystokinin (CCK)-B/gastrin receptor in the gastric glands of guinea pigs [1].
In vitro, A 71623 demonstrates potent agonist activity at the CCK-A receptor. It has an IC50 of 3.7 nM for the CCK-A receptor, indicating high affinity, and exhibits 1200-fold selectivity over the CCK-B receptor. This high selectivity is a key feature that makes A 71623 a valuable research tool for studying the specific role of the CCK-A receptor in appetite regulation, without the confounding effects of CCK-B receptor activation. In cell-based assays, A 71623 can stimulate intracellular signaling pathways downstream of CCK-A receptor activation, such as phospholipase C activation and calcium mobilization. |
| ln Vivo |
A71623 (A-63387; administered intravenously, but not intraperitoneally) decreases food consumption and inhibits the intake of liquid diet in rats that are both satiated and hungry [2]. In Pcp2-ATXN1[30Q]D776;Cck-/- and Pcp2-AXTN1[82Q] mice, A71623 inhibits Purkinje neuron pathology and is linked to motor performance deficits [3]. The locomotor abilities of Pcp2-ATXN2[127Q] SCA2 mice can be enhanced by A71623 [3].
In vivo, A 71623 has been shown to suppress food intake in a variety of animal models. Oral or peripheral administration of A 71623 reduces food consumption in mice, dogs, and monkeys. This effect is mediated through the activation of CCK-A receptors, which trigger satiety signals via the vagus nerve to the brain. The compound's ability to suppress food intake in multiple species highlights its potential utility in studying the neurobiology of appetite and energy balance. It is a valuable tool for investigating the central and peripheral mechanisms that regulate feeding behavior. |
| Enzyme Assay |
Non-cellular in vitro assays for A 71623 typically involve receptor binding studies. A standard protocol involves using membrane preparations from cells expressing recombinant human CCK-A or CCK-B receptors. The membranes are incubated with a radiolabeled ligand, such as [¹²⁵I]CCK-8, and varying concentrations of A 71623. Non-specific binding is determined in the presence of an excess of unlabeled CCK-8. After incubation, the reaction is terminated by rapid filtration, and the radioactivity bound to the membranes is measured. The IC50 or Ki values are calculated from the competition curves using appropriate equations.
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| Cell Assay |
Cellular assays for A 71623 are performed using cell lines expressing the CCK-A receptor, such as CHO cells or HEK293 cells stably transfected with the receptor. Cells are loaded with a calcium-sensitive fluorescent dye (e.g., Fluo-4) and then stimulated with varying concentrations of A 71623. The increase in intracellular calcium concentration is measured using a fluorescence plate reader. The EC50 for calcium mobilization is determined from the concentration-response curve. This assay confirms that A 71623 is a functional agonist capable of activating the receptor and triggering downstream signaling events.
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| Animal Protocol |
Animal/Disease Models: Adult male, SD (SD (Sprague-Dawley)) rat [2]
Doses: 5 μL Route of Administration: Intracerebroventricular (icv) administration, use a 28-gauge injection cannula to infuse A-71623 over 60 seconds in a volume of 5uL Experimental Results: Food intake is diminished and liquid diet intake is inhibited. Animal/Disease Models: ATXN1[30Q]-D776, ATXN1[82Q]-D776, ATXN2[127Q] and WT/FVB/NJ mice[3] Doses: 0.02 mg/kg/day Route of Administration: Contains A71623 (0.02 mg) of osmotic minipumps/kg/day) intraperitoneal(i.p.) implantation Experimental Results: Treatment suppressed Purkinje neuron pathology in ATXN1[30Q]D776;Cck-/- mice and ATXN1[82Q] mice. Improved exercise performance in ATXN2[127Q] mice. In vivo animal studies for A 71623 are conducted to assess its effects on food intake. A typical protocol involves using fasted male Sprague-Dawley rats or mice. Animals are administered A 71623 either intraperitoneally (i.p.) or orally at doses such as 0.01-1 mg/kg. Control animals receive the vehicle. Food intake is measured at various time points post-administration (e.g., 1, 2, 4, and 24 hours). The cumulative food intake is calculated and compared between treatment groups to determine the anorectic effect of the compound. Body weight may also be monitored over longer treatment periods. |
| ADME/Pharmacokinetics |
A 71623 is a peptide-based compound with a high molecular weight of approximately 841 g/mol. As a peptide, it is likely to have poor oral bioavailability due to degradation in the gastrointestinal tract. It is typically administered via injection (i.p. or i.v.) in animal studies. The compound should be stored desiccated at -20°C. Detailed pharmacokinetic parameters for A 71623, such as half-life, clearance, and volume of distribution, have not been extensively reported in the available literature. Its effects on food intake are observed relatively quickly after administration, suggesting a rapid onset of action.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for A 71623 have not been extensively reported. As a research peptide, it is not intended for human use and is strictly for preclinical research purposes. Standard safety precautions should be followed when handling this compound, including the use of personal protective equipment. The compound is typically stored as a powder at -20°C. No specific toxicity data, such as LD50 values, are available in the provided literature.
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| References |
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| Additional Infomation |
A 71623 is a highly selective CCK-A receptor agonist that is widely used as a pharmacological tool to study appetite regulation and the physiology of the CCK system. Its high selectivity for CCK-A over CCK-B receptors makes it a valuable agent for dissecting the distinct roles of these two receptor subtypes. The compound has been instrumental in demonstrating the critical role of CCK-A receptor signaling in mediating the satiating effects of CCK. A 71623 is not a clinically approved drug and has not entered clinical trials. Its primary application is in academic and pharmaceutical research to understand the mechanisms of appetite control and to identify potential targets for anti-obesity therapies.
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| Molecular Formula |
C44H56N8O9
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| Molecular Weight |
840.98
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| Exact Mass |
840.417
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| CAS # |
130408-77-4
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| PubChem CID |
121964
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| Appearance |
White to off-white solid powder
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| LogP |
6.24
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
22
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| Heavy Atom Count |
61
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| Complexity |
1500
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC1=CC=CC=C1NC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](CC2=CC=CC=C2)C(=O)N)NC(=O)[C@H](CC3=CNC4=CC=CC=C43)NC(=O)OC(C)(C)C
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| InChi Key |
KNHCBYMGWWTGSO-ZYADHFCISA-N
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| InChi Code |
InChI=1S/C44H56N8O9/c1-27-15-9-11-19-31(27)50-42(59)46-22-14-13-21-33(39(56)49-35(25-37(53)54)41(58)52(5)36(38(45)55)23-28-16-7-6-8-17-28)48-40(57)34(51-43(60)61-44(2,3)4)24-29-26-47-32-20-12-10-18-30(29)32/h6-12,15-20,26,33-36,47H,13-14,21-25H2,1-5H3,(H2,45,55)(H,48,57)(H,49,56)(H,51,60)(H,53,54)(H2,46,50,59)/t33-,34-,35-,36-/m0/s1
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| Chemical Name |
(3S)-4-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-methylamino]-3-[[(2S)-2-[[(2S)-3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]amino]-6-[(2-methylphenyl)carbamoylamino]hexanoyl]amino]-4-oxobutanoic acid
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| Synonyms |
A-71623 A71623A 71623
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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) |
DMSO : ~50 mg/mL (~59.46 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 | 1.1891 mL | 5.9454 mL | 11.8909 mL | |
| 5 mM | 0.2378 mL | 1.1891 mL | 2.3782 mL | |
| 10 mM | 0.1189 mL | 0.5945 mL | 1.1891 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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