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| Targets |
The primary target of ALB-127158A is the melanin-concentrating hormone 1 (MCH1) receptor, a G protein-coupled receptor that is involved in the regulation of feeding behavior, energy homeostasis, and body weight. ALB-127158A acts as a potent and highly selective antagonist of the MCH1 receptor, with a Ki of approximately 7 nM. It shows excellent selectivity over a range of other GPCRs, ion channels, transporters, and the MCH2 receptor. By blocking MCH1 receptor signaling, ALB-127158A reduces food intake and promotes weight loss.
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| ln Vitro |
ALB-127158(a) exhibits good selectivity over a variety of other G protein-coupled receptors (GPCRs), ion channels, and transporters, including the MCH2 receptor, and a strong affinity for the MCH1 receptor (7 nM). ALB-127158(a) has been shown through in vitro functional studies to be a strong and specific MCH1 receptor antagonist [1].
ALB-127158A demonstrates potent in vitro antagonist activity at the MCH1 receptor, with a Ki of approximately 7 nM. It shows excellent selectivity over a range of other GPCRs, ion channels, and transporters. However, detailed cellular activity data, such as IC50 or EC50 values for inhibition of MCH1-mediated signaling, are not extensively reported in the available literature. |
| ln Vivo |
In a mouse model of diet-induced obesity (DIO), ALB-127158(a) significantly and consistently lowered body weight and food intake in the range of 5-15 mg/kg daily. Weight loss is mostly attributable to a reduction in fat content. In rats fed a high-fat diet (HFD), ALB-127158(a) generated considerable weight loss and food consumption at oral doses as low as 1.25 mg/kg. Oral dosages > 1.25 mg/kg resulted in body weight losses > 6%, with maximal body weight losses of roughly 10% recorded in rats at doses of 10 mg/kg. ALB-127158(a) is readily absorbed following single and multiple oral doses (median tmax attained within 1 to 3 hours postdose in lean and overweight/obese participants), There is a trend of decreasing with dosage, showing that the absorption rate of ALB-127158(a) is slower at lower doses. The mean half-life (t1/2) of ALB-127158(a) is 18 to 21 hours following a single dose. Slightly longer mean t1/2 estimations of roughly 26 hours were observed after numerous doses in overweight/obese patients; steady-state plasma ALB-127158(a) was attained within 6 to 8 days after dosing [1].
ALB-127158A has demonstrated significant weight loss in rodents in preclinical studies. These in vivo findings support the potential of MCH1 receptor antagonists for the treatment of obesity. However, specific in vivo efficacy data, including animal models, dosing regimens, and pharmacokinetic-pharmacodynamic relationships, are not extensively detailed in the available literature. |
| Enzyme Assay |
In vitro receptor binding assays for ALB-127158A typically involve measuring its displacement of a radiolabeled MCH1 receptor ligand from membrane preparations expressing the receptor. The receptor is incubated with a radiolabeled ligand in the presence of varying concentrations of ALB-127158A. The Ki for displacement is calculated from the competition curve, with ALB-127158A showing a Ki of approximately 7 nM.
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| Cell Assay |
In vitro cellular assays for ALB-127158A are performed in cells expressing the MCH1 receptor to assess its antagonist activity. Cells are treated with ALB-127158A in the presence or absence of an MCH1 receptor agonist, and receptor-mediated signaling pathways, such as calcium mobilization or inhibition of cAMP production, are measured. The compound's ability to block agonist-induced effects is assessed.
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| Animal Protocol |
In vivo animal studies with ALB-127158A have been performed in rodent models of obesity to evaluate its effects on body weight and food intake. In these studies, ALB-127158A is administered systemically, and body weight and food consumption are monitored over time. The compound produced significant weight loss in rodents. However, specific protocols are not extensively detailed in the available literature.
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| ADME/Pharmacokinetics |
ALB-127158A has a molecular weight of 404.44 and a molecular formula of C23H21FN4O2. It is a GPCR/G protein-related compound. The compound is stable when stored at -20°C. However, detailed pharmacokinetic parameters such as absorption, distribution, metabolism, excretion, half-life, and bioavailability are not extensively reported in the available literature.
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| Toxicity/Toxicokinetics |
Comprehensive toxicology data for ALB-127158A are not extensively reported. The compound is classified as a research-use-only chemical and is not intended for human consumption. As an MCH1 receptor antagonist, it may have effects on feeding behavior and energy homeostasis that could contribute to toxicity at high concentrations. Specific toxicological data, including acute toxicity, genotoxicity, and target organ effects, are not reported in the available literature.
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| References | |
| Additional Infomation |
ALB-127158A is a research-grade compound not approved for clinical use. Its primary application is as a pharmacological tool for studying the MCH1 receptor and its role in the regulation of feeding behavior and body weight. The compound was developed for the potential treatment of obesity, as preclinical studies demonstrated significant weight loss in rodents. Its high selectivity for MCH1 over other GPCRs makes it a valuable tool for dissecting MCH1 receptor function.
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| Molecular Formula |
C23H21FN4O2
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| Molecular Weight |
404.436848402023
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| Exact Mass |
404.16
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| Elemental Analysis |
C, 68.30; H, 5.23; F, 4.70; N, 13.85; O, 7.91
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| CAS # |
1173154-32-9
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| PubChem CID |
44193892
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| Appearance |
White to off-white solid powder
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| LogP |
1.7
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
713
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VUUUHLIHQHVLLE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H21FN4O2/c1-27-21-6-8-25-13-20(21)19-5-4-17(10-22(19)27)28-9-7-18(11-23(28)29)30-14-16-3-2-15(24)12-26-16/h2-5,7,9-12,25H,6,8,13-14H2,1H3
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| Chemical Name |
4-[(5-fluoropyridin-2-yl)methoxy]-1-(5-methyl-1,2,3,4-tetrahydropyrido[4,3-b]indol-7-yl)pyridin-2-one
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| Synonyms |
ALB-127158A; ALB 127158A; ALB127158A; ALB-127158(a); ALB127158(a); ALB 127158(a); ALB-127158; ALB 127158; ALB127158;
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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 |
| 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) |
Ethanol : ~2 mg/mL (~4.95 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 | 2.4726 mL | 12.3628 mL | 24.7255 mL | |
| 5 mM | 0.4945 mL | 2.4726 mL | 4.9451 mL | |
| 10 mM | 0.2473 mL | 1.2363 mL | 2.4726 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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