| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Kd: ∼0.5 nM (GPR171)[1]
BigLEN (mouse) specifically targets GPR171, an orphan G protein-coupled receptor that is expressed in the brain. It acts as a high-affinity agonist with a Kd of approximately 0.5 nM. Activation of GPR171 by BigLEN inhibits the release of glutamate onto parvocellular neurons of the paraventricular nucleus, a process dependent upon the activation of postsynaptic G proteins. |
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| ln Vitro |
In vitro, BigLEN (mouse) is a potent and selective agonist for GPR171. Its high affinity for the receptor (Kd ~0.5 nM) confirms its role as the endogenous ligand. It is used in cell-based assays to study GPR171-mediated signaling pathways and to investigate the receptor's pharmacology.
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| ln Vivo |
In vivo, BigLEN (mouse) plays a key role in regulating feeding behavior and energy homeostasis in mice. It inhibits the release of glutamate in the paraventricular nucleus, which is a critical brain region for appetite control. This action contributes to its role in the central regulation of food intake and metabolism.
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| Enzyme Assay |
For non-cellular in vitro receptor binding assays, BigLEN (mouse) is characterized using radioligand binding techniques with membrane preparations from cells expressing GPR171. These assays determine its binding affinity (Kd ~0.5 nM) and confirm its specificity for GPR171. Such studies are essential for identifying and characterizing ligand-receptor interactions.
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| Cell Assay |
For in vitro cellular assays, the activity of BigLEN (mouse) is evaluated in cells expressing GPR171. A typical functional assay measures the activation of downstream signaling pathways, such as the inhibition of cAMP accumulation or the mobilization of intracellular calcium, depending on the receptor's coupling. These assays confirm its agonistic activity and are used to study receptor pharmacology.
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| Animal Protocol |
In vivo animal studies with BigLEN (mouse) are typically conducted in mouse models to investigate its role in the regulation of food intake and metabolism. It is often administered via intracerebroventricular (ICV) injection to target the central nervous system directly. Its effects on feeding behavior and neuronal activity are then assessed.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for BigLEN (mouse) are not applicable as it is a research tool, not a therapeutic agent. As a neuropeptide, its half-life in the circulation is expected to be short due to rapid degradation. For research purposes, it is typically administered directly into the brain (e.g., ICV) to bypass systemic clearance and ensure it reaches its target receptors in the central nervous system.
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| Toxicity/Toxicokinetics |
Toxicological data for BigLEN (mouse) are not applicable. As a research compound, it is intended for laboratory use only and not for human therapeutic applications. Its safety profile has not been established for clinical use. At the concentrations used in research, it is generally considered to have low toxicity, but standard laboratory safety practices should always be followed.
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| References | |
| Additional Infomation |
BigLEN (mouse) is a potent and selective endogenous agonist for the orphan G protein-coupled receptor GPR171, with a Kd of ~0.5 nM. It is a proSAAS-derived neuropeptide that regulates food intake and metabolism in mice by inhibiting glutamate release in the paraventricular nucleus. It is a key research tool for studying GPR171 function in the central nervous system.
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| Molecular Formula |
C78H130N24O22
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|---|---|
| Molecular Weight |
1756.01441717148
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| Exact Mass |
1754.979
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| CAS # |
501036-69-7
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| Related CAS # |
BigLEN(mouse) TFA
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| PubChem CID |
131648250
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| Appearance |
White to off-white solid powder
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| LogP |
-8
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| Hydrogen Bond Donor Count |
20
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| Hydrogen Bond Acceptor Count |
25
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| Rotatable Bond Count |
49
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| Heavy Atom Count |
124
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| Complexity |
3890
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| Defined Atom Stereocenter Count |
16
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| SMILES |
C(N1CCC[C@H]1C(=O)O)([C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](C)NC([C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CCC(=O)N)NC([C@@H]1CCCN1C(=O)[C@H](CO)NC([C@@H]1CCCN1C(=O)[C@H](CC(=O)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](N)CC(C)C)=O)=O)=O)=O
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| InChi Key |
UEWHHQZTIIRRRA-REWHPCPNSA-N
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| InChi Code |
InChI=1S/C78H130N24O22/c1-39(2)34-44(79)62(109)91-48(24-26-60(106)107)66(113)96-51(37-59(81)105)73(120)99-30-12-20-55(99)70(117)97-52(38-103)74(121)100-31-13-19-54(100)69(116)93-47(23-25-58(80)104)63(110)89-43(8)71(118)98-29-11-18-53(98)68(115)88-42(7)61(108)90-45(16-9-27-86-77(82)83)64(111)92-46(17-10-28-87-78(84)85)65(112)94-49(35-40(3)4)67(114)95-50(36-41(5)6)72(119)101-32-14-21-56(101)75(122)102-33-15-22-57(102)76(123)124/h39-57,103H,9-38,79H2,1-8H3,(H2,80,104)(H2,81,105)(H,88,115)(H,89,110)(H,90,108)(H,91,109)(H,92,111)(H,93,116)(H,94,112)(H,95,114)(H,96,113)(H,97,117)(H,106,107)(H,123,124)(H4,82,83,86)(H4,84,85,87)/t42-,43-,44-,45-,46-,47-,48-,49-,50-,51-,52-,53-,54-,55-,56-,57-/m0/s1
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| Chemical Name |
(2S)-1-[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-5-amino-2-[[(2S)-1-[(2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]-4-oxobutanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxypropanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxylic 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: 100 mg/mL (56.95 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 | 0.5695 mL | 2.8474 mL | 5.6947 mL | |
| 5 mM | 0.1139 mL | 0.5695 mL | 1.1389 mL | |
| 10 mM | 0.0569 mL | 0.2847 mL | 0.5695 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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