| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
EC50: 1.6 nM (GPR171)[1]
Targets GPR171 (formerly GPR173) as a potent and selective agonist. It is a Galphai/o-coupled receptor, and its activation by BigLEN leads to downstream signaling events, including the inhibition of adenylate cyclase activity and the phosphorylation of ERK1/2. GPR171 has been implicated in regulating body weight, feeding behavior, and neurite outgrowth. |
|---|---|
| ln Vitro |
In vitro, BigLEN(rat) is a potent agonist, exhibiting an EC50 of 1.6 nM for GPR171 activation. It has been shown to promote the outgrowth of neurites (new projections from nerve cells) in Neuro2A cells and is a potent GPR171 agonist. This peptide does not activate the related GPR83, confirming its selectivity.
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| ln Vivo |
In vivo, BigLEN(rat) has been shown to regulate body weight in mice. As a potent agonist of GPR171, its central or peripheral administration can influence metabolic parameters. It is a key tool for exploring the role of the GPR171 receptor in the brain's control of feeding, energy expenditure, and glucose homeostasis.
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| Enzyme Assay |
Cell-free radioligand binding assays for GPR171 are performed using membranes from cells that express the receptor. The membranes are incubated with a radiolabeled form of BigLEN and increasing concentrations of the unlabeled peptide to determine its binding affinity (Ki). These assays are often used in receptor characterization and drug discovery.
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| Cell Assay |
Functional activity is typically assessed by measuring the inhibition of forskolin-stimulated cAMP accumulation. Cells expressing GPR171 are treated with BigLEN(rat) in the presence of forskolin. The amount of intracellular cAMP is then measured using a competitive immunoassay or chemiluminescent detection. The EC50 value of 1.6 nM is derived from this type of assay.
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| Animal Protocol |
No specific animal studies for BigLEN(rat) are publicly detailed. A common protocol would be to administer the peptide centrally (intracerebroventricularly, ICV) or peripherally (intraperitoneally, IP) in mice. Food intake and body weight would be measured at multiple time points post-injection. Changes in metabolic rate or activity could also be assessed.
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| ADME/Pharmacokinetics |
Detailed PK data for BigLEN(rat) is not publicly available. As a peptide, it is not orally bioavailable and is expected to be rapidly degraded by proteases in vivo, leading to a short half-life. It is typically administered via injection in research settings. Its molecular weight is 1745.98, and it has poor predicted LogP of -9.3, reflecting its hydrophilic nature.
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| Toxicity/Toxicokinetics |
No toxicity data is publicly available for BigLEN(rat). As an endogenous peptide agonist, it is not considered toxic in its physiological context. However, chronic or high-dose activation of its receptor could potentially lead to metabolic or neurological side effects. In research use, no overt toxicities have been reported.
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| References | |
| Additional Infomation |
BigLEN(rat) is a research-grade peptide and is not approved for clinical use. It is a vital pharmacological tool for studying the emerging biology of the GPR171 receptor. This receptor is considered a potential drug target for the treatment of metabolic disorders, including obesity, and for neuropsychiatric conditions such as pain and anxiety.
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| Molecular Formula |
C76H128N24O23
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|---|---|
| Molecular Weight |
1745.97653675079
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| Exact Mass |
1744.958
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| CAS # |
369377-66-2
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| Related CAS # |
BigLEN(rat) TFA
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| PubChem CID |
131648251
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| Appearance |
White to off-white solid powder
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| LogP |
-9.3
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| Hydrogen Bond Donor Count |
22
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| Hydrogen Bond Acceptor Count |
26
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| Rotatable Bond Count |
51
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| Heavy Atom Count |
123
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| Complexity |
3820
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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(=O)[C@H](CO)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](N)CC(C)C)=O)=O)=O
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| InChi Key |
IPOOBASOJFKEAK-GTJGPZIJSA-N
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| InChi Code |
InChI=1S/C76H128N24O23/c1-37(2)31-42(77)60(108)89-46(22-24-58(105)106)64(112)93-48(34-57(79)104)66(114)95-50(35-101)67(115)96-51(36-102)72(120)98-28-12-18-53(98)69(117)91-45(21-23-56(78)103)61(109)87-41(8)70(118)97-27-11-17-52(97)68(116)86-40(7)59(107)88-43(15-9-25-84-75(80)81)62(110)90-44(16-10-26-85-76(82)83)63(111)92-47(32-38(3)4)65(113)94-49(33-39(5)6)71(119)99-29-13-19-54(99)73(121)100-30-14-20-55(100)74(122)123/h37-55,101-102H,9-36,77H2,1-8H3,(H2,78,103)(H2,79,104)(H,86,116)(H,87,109)(H,88,107)(H,89,108)(H,90,110)(H,91,117)(H,92,111)(H,93,112)(H,94,113)(H,95,114)(H,96,115)(H,105,106)(H,122,123)(H4,80,81,84)(H4,82,83,85)/t40-,41-,42-,43-,44-,45-,46-,47-,48-,49-,50-,51-,52-,53-,54-,55-/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)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 0.5727 mL | 2.8637 mL | 5.7274 mL | |
| 5 mM | 0.1145 mL | 0.5727 mL | 1.1455 mL | |
| 10 mM | 0.0573 mL | 0.2864 mL | 0.5727 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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