| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
KB: ~100 nM (CRF2 receptor)[2] EC50: 140 nM (CRF1 receptor)[2]
Corticotropin-releasing factor receptor type 1 (CRF1) and type 2 (CRF2). alpha-Helical CRF(9-41) is a competitive antagonist of both CRF receptors, lacking the intrinsic agonist activity of the full-length CRF peptide. Its mechanism of action is to bind to the receptor and block the binding of endogenous CRF. |
|---|---|
| ln Vitro |
alpha-Helical CRF(9-41) is an antagonist of CRF-stimulated ACTH secretion from rat pituitary cells in vitro. It shows no intrinsic agonist activity, meaning it does not stimulate ACTH release on its own. It is a useful tool for blocking the effects of CRF in a variety of in vitro and in vivo systems.
|
| Enzyme Assay |
A cell-free radioligand binding assay is performed using membrane preparations from rat frontal cortex or pituitary, which are rich in CRF receptors. Membranes are incubated with [125I]-Tyr0-CRF or [125I]-sauvagine and varying concentrations of the test peptide. Bound and free ligands are separated by filtration, and the Ki is calculated.
|
| Cell Assay |
A cellular functional assay is performed using rat anterior pituitary cells in primary culture. Cells are seeded in multi-well plates and pre-incubated with alpha-Helical CRF(9-41). The cells are then stimulated with CRF, and the amount of ACTH secreted into the medium is measured by a specific radioimmunoassay (RIA) or ELISA. The antagonist's IC50 is determined.
|
| Animal Protocol |
In vivo, alpha-Helical CRF(9-41) is administered intracerebroventricularly (ICV) in rats or other animals to block central CRF receptors. A common endpoint is the blockade of stress-induced behaviors, such as the reduction in exploratory activity in a novel environment. Alternatively, it can be administered intravenously (IV) to block the effects of peripheral CRF, such as the increase in plasma ACTH and corticosterone.
|
| ADME/Pharmacokinetics |
Not reported. As a peptide, alpha-Helical CRF(9-41) is susceptible to rapid enzymatic degradation in the bloodstream, resulting in a very short half-life. Therefore, for in vivo studies it is often administered via continuous infusion or directly into the brain (ICV) to achieve sustained receptor blockade.
|
| Toxicity/Toxicokinetics |
Not reported. As a research peptide, formal toxicology is unavailable. Its use as a tool to block CRF receptors is well-established, and at the doses commonly used in animal studies, it is generally considered safe for acute experiments.
|
| References |
|
| Additional Infomation |
alpha-Helical CRF(9-41) has been widely used for over three decades to elucidate the physiological functions of CRF. It is a classic pharmacological tool that helped define the role of CRF as a key mediator of the stress response, both as a hormone in the pituitary and as a neurotransmitter in the brain. Its alpha-helical structure is critical for its antagonist activity, distinguishing it from the native peptide.
|
| Molecular Formula |
C166H274N46O53S2
|
|---|---|
| Molecular Weight |
3826.35819673538
|
| Exact Mass |
3824.963
|
| CAS # |
90880-23-2
|
| PubChem CID |
90479767
|
| Appearance |
White to off-white solid powder
|
| LogP |
-11.6
|
| Hydrogen Bond Donor Count |
54
|
| Hydrogen Bond Acceptor Count |
60
|
| Rotatable Bond Count |
137
|
| Heavy Atom Count |
267
|
| Complexity |
9070
|
| Defined Atom Stereocenter Count |
34
|
| SMILES |
S(C)CC[C@@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@@H](C)C(N[C@H](C(N[C@@H](C)C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@@H](C)C(N[C@@H](CCC(=O)O)C(N[C@@H](CCC(N)=O)C(N[C@@H](C)C(N[C@@H](C)C(N[C@H](C(N[C@@H](CC(N)=O)C(N[C@@H](CCCNC(=N)N)C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N)=O)C)=O)CCC(=O)O)=O)CCC(=O)O)=O)CC(C)C)=O)CC(C)C)=O)CC(C)C)=O)=O)=O)CC(C)C)=O)=O)=O)=O)=O)=O)CCC(=O)O)=O)CCC(N)=O)=O)CCC(=O)O)=O)=O)CCCCN)=O)=O)CCSC)=O)CCC(=O)O)=O)CC(C)C)=O)NC([C@H](CCC(=O)O)NC([C@H](CCCNC(=N)N)NC([C@H](CC(C)C)NC([C@H](CC(C)C)NC([C@H](CC1=CNC=N1)NC([C@H](CC1C=CC=CC=1)NC([C@H]([C@@H](C)O)NC([C@H](CC(C)C)NC([C@H](CC(=O)O)N)=O)=O)=O)=O)=O)=O)=O)=O)=O
|
| InChi Key |
PNGVJHODDQMQKT-GVKLFNHCSA-N
|
| InChi Code |
InChI=1S/C166H274N46O53S2/c1-77(2)63-109(156(257)210-119(74-122(171)216)162(263)191-97(37-32-60-179-166(175)176)145(246)203-113(67-81(9)10)157(258)207-114(68-82(11)12)158(259)206-112(66-80(7)8)155(256)197-105(45-54-128(227)228)149(250)194-100(40-49-123(217)218)140(241)181-85(17)132(172)233)201-137(238)87(19)182-133(234)86(18)183-141(242)98(38-47-120(169)214)192-147(248)102(42-51-125(221)222)188-136(237)90(22)185-142(243)101(41-50-124(219)220)195-146(247)99(39-48-121(170)215)193-148(249)103(43-52-126(223)224)189-135(236)89(21)184-139(240)95(35-29-30-58-167)187-134(235)88(20)186-143(244)107(56-61-266-24)199-151(252)106(46-55-129(229)230)198-154(255)110(64-78(3)4)204-152(253)108(57-62-267-25)200-150(251)104(44-53-127(225)226)196-144(245)96(36-31-59-178-165(173)174)190-153(254)111(65-79(5)6)205-159(260)115(69-83(13)14)208-161(262)118(72-93-75-177-76-180-93)209-160(261)117(71-92-33-27-26-28-34-92)211-164(265)131(91(23)213)212-163(264)116(70-84(15)16)202-138(239)94(168)73-130(231)232/h26-28,33-34,75-91,94-119,131,213H,29-32,35-74,167-168H2,1-25H3,(H2,169,214)(H2,170,215)(H2,171,216)(H2,172,233)(H,177,180)(H,181,241)(H,182,234)(H,183,242)(H,184,240)(H,185,243)(H,186,244)(H,187,235)(H,188,237)(H,189,236)(H,190,254)(H,191,263)(H,192,248)(H,193,249)(H,194,250)(H,195,247)(H,196,245)(H,197,256)(H,198,255)(H,199,252)(H,200,251)(H,201,238)(H,202,239)(H,203,246)(H,204,253)(H,205,260)(H,206,259)(H,207,258)(H,208,262)(H,209,261)(H,210,257)(H,211,265)(H,212,264)(H,217,218)(H,219,220)(H,221,222)(H,223,224)(H,225,226)(H,227,228)(H,229,230)(H,231,232)(H4,173,174,178)(H4,175,176,179)/t85-,86-,87-,88-,89-,90-,91+,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,107-,108-,109-,110-,111-,112-,113-,114-,115-,116-,117-,118-,119-,131-/m0/s1
|
| Chemical Name |
(4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-amino-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-4-methylsulfanylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]-4-methylsulfanylbutanoyl]amino]propanoyl]amino]hexanoyl]amino]propanoyl]amino]-5-oxopentanoic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O: 50 mg/mL (13.07 mM)
|
|---|---|
| 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 | 0.2613 mL | 1.3067 mL | 2.6134 mL | |
| 5 mM | 0.0523 mL | 0.2613 mL | 0.5227 mL | |
| 10 mM | 0.0261 mL | 0.1307 mL | 0.2613 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
