| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
UFP-101 TFA targets the nociceptin/orphanin FQ (NOP) opioid receptor. It is a potent, selective, and competitive antagonist with a pKi of 10.24 (Ki of 0.06 nM). It shows high selectivity, with over 3000-fold selectivity against δ, μ, and κ opioid receptors. It demonstrates high affinity in CHO cells expressing the human receptor.
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| ln Vitro |
In vitro, UFP-101 TFA acts as a potent and selective antagonist of the NOP receptor. It has a pKi of 10.24 (Ki of 0.06 nM) and shows over 3000-fold selectivity against δ, μ, and κ opioid receptors. It demonstrates high affinity in CHO cells expressing the human receptor.
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| ln Vivo |
Mice subjected to the forced swimming test (FST) showed a strong immediate and dose-dependent antidepressant-like response when given UFP-101 TFA[1].
In vivo, UFP-101 TFA exhibits antidepressant-like effects. Specific in vivo activity data, such as its effects in the tail withdrawal test, indicate that it can antagonize the effects of N/OFQ. |
| Enzyme Assay |
Non-cellular receptor binding assays for UFP-101 TFA involve measuring its binding affinity to the NOP receptor using radioligand binding techniques. The compound is incubated with membranes expressing the NOP receptor and a labeled ligand, and the displacement is quantified to determine the pKi value.
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| Cell Assay |
In vitro cellular assays for UFP-101 TFA are performed using cells expressing the NOP receptor to assess receptor antagonism. The compound's ability to inhibit NOP receptor-mediated signaling, such as cAMP modulation, is measured.
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| Animal Protocol |
In vivo animal experiments for UFP-101 TFA would be conducted in animal models to study its antidepressant-like effects. The compound would be administered via appropriate routes, and behavioral tests, such as the forced swim test or tail suspension test, would be used to assess its efficacy.
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| ADME/Pharmacokinetics |
UFP-101 TFA is the trifluoroacetate salt of the synthetic peptide [Nphe¹,Arg¹⁴,Lys¹⁵]N/OFQ-NH₂. Its CAS number is not detailed in the search results. It has a molecular weight of 2309.7. It is a synthetic peptide.
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| Toxicity/Toxicokinetics |
Toxicological data for UFP-101 TFA are not detailed in the search results. As a research peptide, its safety profile has not been extensively characterized. It is intended for research use only and not for human consumption.
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| References |
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| Additional Infomation |
UFP-101 TFA is a potent, selective, and competitive antagonist of the NOP receptor. It has a pKi of 10.24 and shows over 3000-fold selectivity against δ, μ, and κ opioid receptors. UFP-101 TFA exhibits antidepressant-like effects. No clinical trial or regulatory approval information is available.
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| Molecular Formula |
C84H139F3N32O23
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|---|---|
| Molecular Weight |
2022.19
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| Related CAS # |
UFP-101;849024-68-6
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| Appearance |
White to off-white solid powder
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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) |
H2O :~130 mg/mL (~64.29 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (49.45 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.4945 mL | 2.4726 mL | 4.9451 mL | |
| 5 mM | 0.0989 mL | 0.4945 mL | 0.9890 mL | |
| 10 mM | 0.0495 mL | 0.2473 mL | 0.4945 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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