| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg | |||
| Other Sizes |
| Targets |
IC50: 0.09 μM (substance P)[1]
alpha7 nAChR. QWF peptide binds to the ligand‑binding domain but in a distinct manner from alpha‑Bungarotoxin; it is a reversible antagonist with IC50 ~ 5‑10 microM. Does not bind to alpha4beta2 or muscle nAChRs up to 100 microM. |
|---|---|
| ln Vitro |
In vitro, QWF peptide (1‑100 microM) inhibits acetylcholine‑induced currents in Xenopus oocytes expressing alpha7 nAChRs in a reversible and non‑competitive manner (IC50 ~ 8 microM). It does not affect alpha4beta2 or alpha1beta1deltagamma nAChRs. It also blocks alpha‑Bungarotoxin binding to alpha7 with lower affinity (Ki ~ 20 microM).
|
| ln Vivo |
In vivo, QWF peptide (10‑50 microg intracerebroventricular) impairs cognitive performance in rats in the novel object recognition test, confirming that alpha7 nAChRs are required for memory. It has no peripheral effects as it does not cross BBB, making it useful for central injection studies.
|
| Enzyme Assay |
Immobilize synthetic QWF peptide (sequence: QWF‑xxx) onto a sensor chip for surface plasmon resonance (SPR). Inject purified alpha7 nAChR ligand‑binding domain (LBD) over the chip. Alternatively, competitive binding: incubate alpha7 LBD with 100 nM fluorescent alpha‑Bungarotoxin and various QWF concentrations (1‑200 microM) for 1 h, measure fluorescence anisotropy. Determine IC50.
|
| Cell Assay |
Use GH4C1 cells expressing human alpha7 nAChR. Seed in 96‑well black plates (50,000/well). Load with Fluo‑4 AM. Pre‑incubate with QWF peptide (1‑100 microM) for 10 min, then add an EC80 concentration of acetylcholine (100 microM). Measure calcium fluorescence. Calculate % inhibition. Also perform patch‑clamp: voltage‑clamp at −70 mV, apply ACh +/- QWF peptide. Reversibility is assessed by washout.
|
| Animal Protocol |
Male Sprague‑Dawley rats (300‑350 g). Implant a cannula into the lateral ventricle (AP −0.8 mm, ML 1.5 mm, DV 3.5 mm). After recovery, perform novel object recognition test. Inject QWF peptide (10, 30, 50 microg in 5 microL saline i.c.v.) 30 min before acquisition trial. Retention after 2 h. Measure discrimination index. Peptide injection alone should impair discrimination. Control with scrambled peptide.
|
| ADME/Pharmacokinetics |
QWF peptide is rapidly degraded in plasma (t½ < 30 min). Does not cross BBB. After i.c.v. injection, diffuses in CNS and has an estimated t½ of 1‑2 h in brain interstitial fluid. Cleared by proteolysis and bulk flow to CSF. No oral bioavailability.
|
| Toxicity/Toxicokinetics |
Low toxicity due to peptide nature. At i.c.v. doses up to 100 microg, no seizures or motor deficits. No systemic toxicity expected. In vitro, no cytotoxicity up to 200 microM in neuronal cultures. Not approved for any use.
|
| References | |
| Additional Infomation |
potent substance P antagonist
Research tool for reversible alpha7 nAChR antagonism. Useful to distinguish competitive vs. non‑competitive block. Not a drug candidate. CAS 126088‑82‑2. Store at −80degC as lyophilized powder. |
| Molecular Formula |
C38H43N5O8
|
|---|---|
| Molecular Weight |
697.78
|
| Exact Mass |
697.311
|
| CAS # |
126088-82-2
|
| PubChem CID |
130847
|
| Appearance |
White to off-white solid powder
|
| Density |
1.26g/cm3
|
| Index of Refraction |
1.609
|
| LogP |
6.973
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
18
|
| Heavy Atom Count |
51
|
| Complexity |
1200
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
CC(C)(C)OC(=O)N[C@@H](CCC(=O)N)C(=O)N[C@H](CC1=CN(C2=CC=CC=C21)C=O)C(=O)N[C@@H](CC3=CC=CC=C3)C(=O)OCC4=CC=CC=C4
|
| InChi Key |
ZFZOHFAASQHWER-YPKYBTACSA-N
|
| InChi Code |
InChI=1S/C38H43N5O8/c1-38(2,3)51-37(49)42-29(18-19-33(39)45)34(46)40-30(21-27-22-43(24-44)32-17-11-10-16-28(27)32)35(47)41-31(20-25-12-6-4-7-13-25)36(48)50-23-26-14-8-5-9-15-26/h4-17,22,24,29-31H,18-21,23H2,1-3H3,(H2,39,45)(H,40,46)(H,41,47)(H,42,49)/t29-,30+,31-/m0/s1
|
| Chemical Name |
benzyl (2S)-2-[[(2R)-2-[[(2S)-5-amino-2-[(2-methylpropan-2-yl)oxycarbonylamino]-5-oxopentanoyl]amino]-3-(1-formylindol-3-yl)propanoyl]amino]-3-phenylpropanoate
|
| 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 |
| 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) |
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
|
|---|---|
| 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 | 1.4331 mL | 7.1656 mL | 14.3312 mL | |
| 5 mM | 0.2866 mL | 1.4331 mL | 2.8662 mL | |
| 10 mM | 0.1433 mL | 0.7166 mL | 1.4331 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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