| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
NMDA Receptor
None (inactive control). Tat-NR2Baa is an inactive peptide that does not bind to PSD‑95. The active peptide, Tat-NR2B9c, targets the interaction between the NMDA receptor subunit NR2B (GluN2B) and PSD‑95. By blocking this protein‑protein interaction, Tat-NR2B9c prevents excitotoxic signaling without blocking NMDA receptor ion flux. Tat-NR2Baa, with its double‑point mutation (e.g., S→A, V→A), does not bind PSD‑95. |
|---|---|
| ln Vitro |
PSD-95 and NR2B subunit interactions are not affected by Tat-NR2BAA (125 ng; 20 mins). On the other hand, rats pretreated with the disruptive peptide Tat-NR2B9c in lumbar dorsal horn tissue exhibit a significant decrease in PSD-95 coimmunoprecipitation with NR2B subunits[1]. The control group for Tat-NR2B9c is Tat-NR2Baa (125 ng or 1.25 μg; 20 minutes before collection of lumbar dorsal horn tissue). Tat-NR2B9c causes a strong and noticeable post-discharge decrease, which suggests that the cell is hyperexcitable. However, even at a dose 100× higher than the active peptide Tat-NR2B9c, Tat-NR2Baa had no impact [1]. In the Co-IP test, the control group is Tat-NR2Baa (1 μM; pre-treatment 1 hour). In hippocampal neurons, the coupling of NR2B to PSD-95 is more vulnerable to disruption than NR2A/PSD95, and Tat-NR2B9c (1 μM) impairs the NR2B/PSD95 interaction[2].
In vitro, Tat-NR2Baa does not disrupt the NR2B‑PSD‑95 interaction in co‑immunoprecipitation assays, whereas Tat-NR2B9c does. It does not reduce NMDA‑induced NO production or protect against excitotoxicity in neuronal cultures. It has no effect on PSD‑95 clustering or on NMDA receptor‑mediated signaling. As a control, it shows no activity in any assay where Tat-NR2B9c is active. |
| ln Vivo |
In vivo, Tat-NR2Baa (administered intravenously or intracerebroventricularly) has no effect on infarct volume in the middle cerebral artery occlusion (MCAO) model of stroke, unlike Tat-NR2B9c, which reduces infarct size. It does not affect pain thresholds in neuropathic pain models. It is used as a control to confirm that the effects of Tat-NR2B9c are due to specific disruption of the NR2B‑PSD‑95 interaction.
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| Enzyme Assay |
Not applicable. For a negative control peptide, no binding activity is expected. To confirm the lack of binding, a pull‑down assay can be performed: GST‑PSD‑95 (1 ug) is immobilized on glutathione‑Sepharose beads and incubated with lysates of cells expressing NR2B, in the presence or absence of Tat-NR2Baa (1‑100 uM). The beads are washed, and bound NR2B is detected by Western blot. Tat-NR2Baa does not reduce binding, whereas Tat-NR2B9c does.
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| Cell Assay |
For cellular assays, primary cortical neurons (DIV 12‑14) are seeded in 96‑well plates (50,000 cells/well). Cells are treated with Tat-NR2Baa (0.1‑10 uM) or Tat-NR2B9c (0.1‑10 uM) for 2‑4 hours. For excitotoxicity studies, cells are exposed to NMDA (50 uM, 15 min) in the presence of the peptides. Cell viability is measured by MTT or LDH release 24 h later. Tat-NR2Baa does not protect against NMDA‑induced cell death, whereas Tat-NR2B9c does. For co‑immunoprecipitation, cells are treated with peptides, lysed, immunoprecipitated with anti‑NR2B, and blotted for PSD‑95. Tat-NR2Baa does not disrupt co‑IP. For calcium imaging, neurons loaded with Fluo‑4 AM are treated with peptide and then stimulated with NMDA; Tat-NR2Baa does not reduce calcium influx.
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| Animal Protocol |
In vivo studies are performed in male C57BL/6 mice (20‑30 g) or Sprague‑Dawley rats (250‑300 g). Tat-NR2Baa is formulated in sterile saline and administered intravenously (3‑30 nmol/g) or intracerebroventricularly (5‑10 ug/animal) 30‑60 min before the injury or insult. In the MCAO model of stroke, mice undergo 60‑90 min of middle cerebral artery occlusion, followed by 24‑48 h of reperfusion. Tat-NR2Baa is injected at the onset of reperfusion (i.v.). Infarct volume is measured by TTC staining. Tat-NR2Baa has no effect compared to vehicle, while Tat-NR2B9c reduces infarct volume by 40‑60%. In the CCI model of neuropathic pain, Tat-NR2Baa (10‑100 ug IT) does not reverse mechanical allodynia or thermal hyperalgesia. For behavioral testing, the open field test is performed to rule out non‑specific motor effects; Tat-NR2Baa has no effect.
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| ADME/Pharmacokinetics |
As a peptide, Tat-NR2Baa (MW 2474.8, sequence YGRKKRRQRRRxxxxx) is similar to Tat-NR2B9c but with a mutation. It is soluble in water. For in vivo use, it is administered by IV or ICV injection. The half‑life in the blood is short (<30 min) due to proteolysis. The peptide may not cross the BBB efficiently after systemic administration, so ICV administration is preferred for CNS studies.
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| Toxicity/Toxicokinetics |
Preclinical toxicity is low; at doses used (3‑30 nmol/g IV, 10‑100 ug ICV), no adverse effects are observed. The peptide is for research use only.
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| References | |
| Additional Infomation |
Tat-NR2Baa (CAS 847829-41-8) is an inactive control peptide for Tat-NR2B9c. It contains a double‑point mutation in the tSXV motif, which prevents binding to PSD‑95. It is used as a negative control in studies of the NR2B‑PSD‑95 interaction, stroke, and pain. For research use only.
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| Molecular Formula |
C103H184N42O29
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|---|---|
| Molecular Weight |
2474.82707881927
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| Exact Mass |
2474.424
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| CAS # |
847829-41-8
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| Related CAS # |
Tat-NR2Baa TFA
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| PubChem CID |
168012956
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| Appearance |
White to off-white solid powder
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| LogP |
-19.2
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| Hydrogen Bond Donor Count |
48
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| Hydrogen Bond Acceptor Count |
39
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| Rotatable Bond Count |
97
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| Heavy Atom Count |
174
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| Complexity |
5300
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| Defined Atom Stereocenter Count |
20
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| SMILES |
[C@H](CCCNC(N)=N)(C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(N)=N)NC(=O)CNC(=O)[C@@H](N)CC1C=CC(O)=CC=1
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| InChi Key |
JGOHJQLBRJDBTQ-RVYJUWCMSA-N
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| InChi Code |
InChI=1S/C103H184N42O29/c1-7-53(4)78(96(172)140-69(34-36-76(151)152)81(157)128-54(5)79(155)141-71(48-77(153)154)92(168)129-55(6)97(173)174)145-95(171)73(51-147)144-94(170)72(50-146)143-93(169)70(46-52(2)3)142-90(166)62(22-10-13-39-106)133-85(161)63(24-15-41-122-99(111)112)135-87(163)65(26-17-43-124-101(115)116)136-88(164)66(27-18-44-125-102(117)118)138-91(167)68(33-35-74(108)149)139-89(165)67(28-19-45-126-103(119)120)137-86(162)64(25-16-42-123-100(113)114)134-84(160)61(21-9-12-38-105)132-83(159)60(20-8-11-37-104)131-82(158)59(23-14-40-121-98(109)110)130-75(150)49-127-80(156)58(107)47-56-29-31-57(148)32-30-56/h29-32,52-55,58-73,78,146-148H,7-28,33-51,104-107H2,1-6H3,(H2,108,149)(H,127,156)(H,128,157)(H,129,168)(H,130,150)(H,131,158)(H,132,159)(H,133,161)(H,134,160)(H,135,163)(H,136,164)(H,137,162)(H,138,167)(H,139,165)(H,140,172)(H,141,155)(H,142,166)(H,143,169)(H,144,170)(H,145,171)(H,151,152)(H,153,154)(H,173,174)(H4,109,110,121)(H4,111,112,122)(H4,113,114,123)(H4,115,116,124)(H4,117,118,125)(H4,119,120,126)/t53-,54-,55-,58-,59-,60-,61-,62-,63-,64-,65-,66-,67-,68-,69-,70-,71-,72-,73-,78-/m0/s1
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| Chemical Name |
(4S)-4-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]hexanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-oxopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylpentanoyl]amino]-5-[[(2S)-1-[[(2S)-3-carboxy-1-[[(1S)-1-carboxyethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-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 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)
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.4041 mL | 2.0203 mL | 4.0407 mL | |
| 5 mM | 0.0808 mL | 0.4041 mL | 0.8081 mL | |
| 10 mM | 0.0404 mL | 0.2020 mL | 0.4041 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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