| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
NK-2 tachykinin receptor (neurokinin receptor 2); also binds NK-1 and NK-3 with lower affinity.
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|---|---|
| ln Vitro |
MEN 10207 (IC50 range 21-54 nM) in the stomach membrane of cows and SKLKB82#3 cells, a murine fibroblast cell line transfected with cDNA encoding the bovine NK2 receptor, exhibit strong affinity in competitive radioligand binding experiments [3].
MEN 10207 is a selective NK-2 tachykinin receptor blocker with pA2 values of 5.2 (NK-1), 7.9 (NK-2), and 4.9 (NK-3). The compound demonstrates significant activity across these receptors, with highest selectivity for NK-2. It is a peptide-based antagonist used for studying tachykinin receptor pharmacology. |
| ln Vivo |
Substance P is not dose-dependent, though. Furthermore, the long-term reflex-promoting action of gastrocnemius nerve stimulation is likewise efficiently blocked by MEN 10207 [1].
In vivo efficacy data for MEN 10207 is limited. The compound is primarily used as an in vitro tool for studying tachykinin receptor pharmacology and neurokinin signaling. As an NK-2 antagonist, it has potential applications in studying smooth muscle contraction, inflammation, and pain pathways where tachykinins are involved. Further in vivo studies would be needed to assess its therapeutic potential. |
| Enzyme Assay |
In vitro receptor binding assays measure the affinity of MEN 10207 for tachykinin receptors (NK-1, NK-2, NK-3). Membrane preparations from cells expressing recombinant human NK receptors are incubated with radiolabeled tachykinin ligands (e.g., [125I]BH-SP for NK-1, [125I]NKA for NK-2) and varying concentrations of MEN 10207 (typically 0.01 nM to 100 µM). pA2 values are calculated from Schild plot analysis of functional antagonist assays.
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| Cell Assay |
In vitro functional assays are performed using cells expressing NK-1, NK-2, or NK-3 receptors. Cells are pre-incubated with MEN 10207 at varying concentrations (0.01 nM to 100 µM) for 30-60 minutes, then stimulated with appropriate tachykinin agonists (substance P for NK-1, neurokinin A for NK-2, neurokinin B for NK-3). Intracellular calcium mobilization is measured using fluorescent dyes. pA2 values are calculated from dose-response curves using Schild analysis.
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| Animal Protocol |
Animal/Disease Models: Decerebrate, spinalized, unanesthetized female SD (SD (Sprague-Dawley)) rats (250-280 g) [1]
Doses: 7 pmol/10 μL, 70 pmol/10 μL, 700 pmol/10 μL Route of Administration: Sheath Intrathecal administration; Experimental Results: Blocked reflex facilitation by intrathecal neurokinin A, but not substance P, in a dose-dependent manner. In vivo animal model data for MEN 10207 is not extensively reported in the literature. As a research tool for studying tachykinin receptor pharmacology, the compound would typically be evaluated in animal models of smooth muscle contraction, inflammation, or pain. Standard efficacy studies would involve compound administration followed by assessment of appropriate physiological responses. Pharmacokinetic studies would assess bioavailability and tissue distribution. |
| ADME/Pharmacokinetics |
MEN 10207 has a molecular weight of approximately 1200 g/mol. CAS number: 126050-12-2. It is a peptide antagonist. Sequence: 5-Tyr-6,8,9-Trp-10-Arg-Neurokinin A (4-10). Store as a lyophilized powder at -20°C. Soluble in water or buffer. For in vivo use, formulate in sterile saline or PBS. The peptide is stable for up to 1 year when stored desiccated at -20°C.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available for MEN 10207. As a research peptide, it is not intended for human use and has not undergone formal toxicological evaluation. Standard preclinical safety assessments would include cytotoxicity profiling, immunogenicity assessment, and off-target receptor screening. The compound is for research use only.
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| References |
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| Additional Infomation |
MEN 10207 is a research-grade selective NK-2 tachykinin receptor antagonist. It is not approved for clinical use. The compound is a peptide with sequence 5-Tyr-6,8,9-Trp-10-Arg-Neurokinin A (4-10). It is a valuable tool for studying tachykinin receptor pharmacology, smooth muscle contraction, and neurokinin signaling pathways. MEN 10207 is supplied as a lyophilized powder with high purity.
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| Molecular Formula |
C57H68N14O10
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|---|---|
| Molecular Weight |
1109.25
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| Exact Mass |
1108.524
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| CAS # |
126050-12-2
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| PubChem CID |
25079030
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.711
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| LogP |
3.11
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| Hydrogen Bond Donor Count |
15
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
28
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| Heavy Atom Count |
81
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| Complexity |
2190
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| Defined Atom Stereocenter Count |
7
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| SMILES |
CC(C)[C@@H](C(=O)N[C@H](CC1=CNC2=CC=CC=C21)C(=O)N[C@H](CC3=CNC4=CC=CC=C43)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N)NC(=O)[C@@H](CC5=CNC6=CC=CC=C65)NC(=O)[C@H](CC7=CC=C(C=C7)O)NC(=O)[C@H](CC(=O)O)N
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| InChi Key |
RLHLZLAKTUPWES-PEURKWGASA-N
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| InChi Code |
InChI=1S/C57H68N14O10/c1-30(2)49(71-55(80)47(25-34-29-65-42-15-8-5-12-38(34)42)69-52(77)44(22-31-17-19-35(72)20-18-31)67-51(76)39(58)26-48(73)74)56(81)70-46(24-33-28-64-41-14-7-4-11-37(33)41)54(79)68-45(23-32-27-63-40-13-6-3-10-36(32)40)53(78)66-43(50(59)75)16-9-21-62-57(60)61/h3-8,10-15,17-20,27-30,39,43-47,49,63-65,72H,9,16,21-26,58H2,1-2H3,(H2,59,75)(H,66,78)(H,67,76)(H,68,79)(H,69,77)(H,70,81)(H,71,80)(H,73,74)(H4,60,61,62)/t39-,43-,44-,45+,46+,47+,49-/m0/s1
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| Chemical Name |
(3S)-3-amino-4-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2R)-1-[[(2R)-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-4-oxobutanoic acid
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| Synonyms |
MEN10207; MEN-10207; MEN 10207
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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) |
DMSO : ~50 mg/mL (~45.08 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 | 0.9015 mL | 4.5076 mL | 9.0151 mL | |
| 5 mM | 0.1803 mL | 0.9015 mL | 1.8030 mL | |
| 10 mM | 0.0902 mL | 0.4508 mL | 0.9015 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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