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| 1mg |
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| 5mg |
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| 10mg | |||
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| Targets |
The primary target of Astressin 2B is the CRF2 receptor (corticotropin-releasing factor receptor 2). CRF2 is a G protein-coupled receptor that mediates the effects of corticotropin-releasing factor (CRF) and related peptides. Astressin 2B is a potent and selective antagonist of CRF2, with an IC50 of 1.3 nM. It has low affinity for the CRF1 receptor (IC50 >500 nM), demonstrating high selectivity.
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| ln Vitro |
Astressin 2B is a potent and selective CRF2 antagonist with an IC50 of 1.3 nM for CRF2 and >500 nM for CRF1. It antagonizes CRF2-mediated inhibition of gastric emptying. The compound's high selectivity for CRF2 over CRF1 makes it a valuable tool for studying CRF2-specific functions. It is supplied as a peptide with a purity of >98% and is soluble in water at 1 mg/mL.
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| ln Vivo |
In vivo, Astressin 2B is used to study the physiological and pathological roles of CRF2. By antagonizing CRF2, it can modulate stress responses, anxiety, depression, and gastrointestinal function. It has been shown to antagonize CRF2-mediated inhibition of gastric emptying. Its efficacy would be assessed in animal models of stress-related disorders and gastrointestinal dysfunction.
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| Enzyme Assay |
In vitro binding and functional assays for Astressin 2B are used to characterize its affinity for CRF2 and CRF1. Radioligand binding assays are performed using membranes from cells expressing CRF2 or CRF1, and the compound's ability to displace a labeled CRF ligand is measured. Functional assays measuring CRF2-mediated signaling (e.g., cAMP accumulation) are used to confirm antagonistic activity. The reported IC50 values are 1.3 nM for CRF2 and >500 nM for CRF1.
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| Cell Assay |
Cellular assays for Astressin 2B involve treating CRF2-expressing cells with the compound and measuring inhibition of CRF-induced signaling. Readouts include inhibition of cAMP accumulation or other downstream signaling pathways. The compound's ability to block CRF2-mediated effects confirms its antagonistic activity.
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| Animal Protocol |
In vivo studies with Astressin 2B are performed in animal models to investigate CRF2 function. The compound is typically administered via injection. Its effects on stress responses, anxiety-like behavior, depression-like behavior, and gastrointestinal function are assessed. For example, its ability to antagonize CRF2-mediated inhibition of gastric emptying can be evaluated.
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| ADME/Pharmacokinetics |
Astressin 2B is a peptide with a molecular weight of 4041.69 and a molecular formula of C183H307N49O53. It is a potent and selective CRF2 antagonist with IC50 values of 1.3 nM for CRF2 and >500 nM for CRF1. The compound is supplied as a peptide with a purity of >98% and is soluble in water at 1 mg/mL. It should be stored under recommended conditions. The compound is for research use only and is not intended for human therapeutic use.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available for Astressin 2B in the provided literature. As a research peptide, its safety profile would be an important consideration for in vivo applications. Potential toxicities could be related to its effects on CRF2-mediated stress responses and gastrointestinal function. Standard preclinical safety studies would be required to evaluate its safety for potential therapeutic applications. The compound is for research use only and is not intended for human therapeutic use.
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| References |
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| Additional Infomation |
CRF2 receptor antagonists
Astressin 2B is a potent and selective peptide antagonist of the corticotropin-releasing factor receptor 2 (CRF2). It has IC50 values of 1.3 nM for CRF2 and >500 nM for CRF1. Astressin 2B has a molecular formula of C183H307N49O53 and a molecular weight of 4041.69. It antagonizes CRF2-mediated inhibition of gastric emptying. The compound is a research tool for studying the physiological and pathological roles of CRF2 in stress responses, anxiety, depression, and gastrointestinal function. |
| Molecular Formula |
C183H307N49O53
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|---|---|
| Exact Mass |
4039.28
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| CAS # |
681260-70-8
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| PubChem CID |
56972208
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
10.193
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| Hydrogen Bond Donor Count |
55
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| Hydrogen Bond Acceptor Count |
59
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| Rotatable Bond Count |
138
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| Heavy Atom Count |
285
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| Complexity |
9670
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| Defined Atom Stereocenter Count |
36
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| SMILES |
CCCCC(C(=O)NC(C(C)CC)C(=O)NC(CCC(=O)O)C(=O)NC(C(C)CC)C(=O)NC(CCC(=O)O)C(=O)NC(CCCCN)C(=O)NC(CCC(=O)N)C(=O)NC(CCC(=O)O)C(=O)NC(CCCCN)C(=O)NC(CCC(=O)O)C(=O)NC(CCCCN)C(=O)NC(CCC(=O)N)C(=O)NC(CCC(=O)N)C(=O)NC(C)C(=O)NC1CCC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC1=O)CC(=O)N)CC(=O)N)C(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(CC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)NC(C(C)CC)C(=O)N)NC(=O)C(CCCCN)NC(=O)C(CCCNC(=N)N)NC(=O)C(CC(C)C)NC(=O)C(C)(CC(C)C)NC(=O)C(CC2=CNC=N2)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CO)NC(=O)C(CC(C)C)NC(=O)C(CC(=O)O)NC(=O)C
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| InChi Key |
IVIBPRHVUKMKSX-XJYAKNQHSA-N
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| InChi Code |
InChI=1S/C183H307N49O53/c1-26-30-47-106(203-151(256)107(48-34-39-70-184)204-155(260)112(53-44-75-198-181(194)195)209-169(274)125(80-96(13)14)227-179(284)182(24,87-97(15)16)231-175(280)127(82-105-89-196-91-199-105)222-170(275)126(81-104-45-32-31-33-46-104)221-174(279)132(90-233)226-168(273)124(79-95(11)12)220-173(278)130(85-143(249)250)201-103(23)234)163(268)228-146(100(20)28-3)178(283)216-120(61-69-142(247)248)164(269)229-147(101(21)29-4)177(282)215-119(60-68-141(245)246)161(266)207-109(50-36-41-72-186)153(258)212-115(56-64-135(190)237)158(263)214-118(59-67-140(243)244)160(265)206-110(51-37-42-73-187)154(259)213-117(58-66-139(241)242)159(264)205-108(49-35-40-71-185)152(257)211-114(55-63-134(189)236)157(262)210-113(54-62-133(188)235)150(255)200-102(22)149(254)202-116-57-65-138(240)197-74-43-38-52-111(208-171(276)128(83-136(191)238)224-172(277)129(84-137(192)239)223-162(116)267)156(261)217-121(76-92(5)6)165(270)218-122(77-93(7)8)166(271)219-123(78-94(9)10)167(272)225-131(86-144(251)252)176(281)232-183(25,88-98(17)18)180(285)230-145(148(193)253)99(19)27-2/h31-33,45-46,89,91-102,106-132,145-147,233H,26-30,34-44,47-88,90,184-187H2,1-25H3,(H2,188,235)(H2,189,236)(H2,190,237)(H2,191,238)(H2,192,239)(H2,193,253)(H,196,199)(H,197,240)(H,200,255)(H,201,234)(H,202,254)(H,203,256)(H,204,260)(H,205,264)(H,206,265)(H,207,266)(H,208,276)(H,209,274)(H,210,262)(H,211,257)(H,212,258)(H,213,259)(H,214,263)(H,215,282)(H,216,283)(H,217,261)(H,218,270)(H,219,271)(H,220,278)(H,221,279)(H,222,275)(H,223,267)(H,224,277)(H,225,272)(H,226,273)(H,227,284)(H,228,268)(H,229,269)(H,230,285)(H,231,280)(H,232,281)(H,241,242)(H,243,244)(H,245,246)(H,247,248)(H,249,250)(H,251,252)(H4,194,195,198)/t99-,100-,101-,102-,106-,107-,108-,109-,110-,111-,112-,113-,114-,115-,116-,117-,118-,119-,120-,121-,122-,123-,124-,125-,126+,127-,128-,129-,130-,131-,132-,145-,146-,147-,182-,183-/m0/s1
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| Chemical Name |
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-2,4-dimethylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-6-aminohexanoyl]amino]hexanoyl]amino]-3-methylpentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-5-amino-5-oxopentanoyl]amino]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-5-[[(2S)-6-amino-1-[[(2S)-5-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(3S,6S,9S,18S)-18-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]-3,6-bis(2-amino-2-oxoethyl)-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxohexan-2-yl]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 |
| 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.) |
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.
Link: https://clinicaltrials.gov/ct2/show/NCT01049542
Conditions:Vascular Disease|Heart DiseaseProducts are for research use only; We do not sell to patients
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