| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| Other Sizes |
Purity: ≥98%
| Targets |
PD 90780 targets nerve growth factor (NGF), a neurotrophin that plays a critical role in the survival, development, and function of neurons. The compound binds directly to NGF with a Kd of 25.83 µM and inhibits NGF binding to the extracellular domain of p75^NTR^ with an IC₅₀ of 220 nM. By acting as an NGF antagonist, PD 90780 disrupts NGF-mediated signaling through p75^NTR^.
|
|---|---|
| ln Vitro |
PD 90780 (0.1-100 μM; 2 hours) has an impact on 125I-BDNF's ability to bind to truncatedp75NTR. PD 90780 (100 μM; 2 hours) prevents 125I-NGF from cross-linking to p75NTR [1]. At a dosage of 300 μM, PD 90780 (0-300 μM; 2 hours) decreases TrkA phosphorylation caused by NGF binding [1]. The NGF-p75NTR interaction is inhibited by PD 90780 (0.1-100 μM; 2 h), with IC50 values of 23.1 μM and 1.8 μM in PC12 cells and PC12nnr5 cells, respectively [1].
In vitro, PD 90780 binds to NGF and inhibits its interaction with the p75 neurotrophin receptor. The compound inhibits NGF-p75^NTR^ interaction with IC₅₀ values of 23.1 in PC12 cells and PC12nnr5 cells. By blocking NGF binding to p75^NTR^, PD 90780 modulates NGF-mediated signaling pathways, including those involved in neuronal survival and apoptosis. |
| ln Vivo |
In vivo, PD 90780 has been used to study the role of NGF and p75^NTR^ in various biological processes. As a non-peptidic NGF antagonist, it provides a tool for investigating NGF-mediated signaling in animal models of pain, neurodegeneration, and other conditions.
|
| Enzyme Assay |
In vitro binding assays for NGF antagonism involve incubating NGF with PD 90780 at varying concentrations and measuring the inhibition of NGF binding to p75^NTR^ extracellular domain using ELISA or surface plasmon resonance. IC₅₀ values are calculated from dose-response curves.
|
| Cell Assay |
Cellular assays are performed using PC12 cells or other NGF-responsive cell lines. Cells are treated with PD 90780 at various concentrations in the presence of NGF. NGF-mediated signaling is assessed by measuring downstream effects such as neurite outgrowth, survival, or apoptosis. The inhibition of NGF-induced responses confirms receptor antagonism.
|
| Animal Protocol |
In vivo studies are conducted in animal models of pain, neurodegeneration, or other NGF-related conditions. PD 90780 is administered via appropriate routes, and endpoints are selected based on the specific biological process being investigated.
|
| ADME/Pharmacokinetics |
PD 90780 (molecular weight 362.34, formula C₁₉H₁₄N₄O₄) is a small-molecule compound. It is soluble in 1 equivalent NaOH (7.25 mg/mL with sonication). The compound is stable as a powder at -20°C for 3 years and at 4°C for 2 years.
|
| Toxicity/Toxicokinetics |
Preclinical toxicity studies of PD 90780 have been limited, as the compound is primarily used as a research tool. No significant toxicity has been reported in the available literature. The compound's safety profile supports its use for studying NGF biology.
|
| References |
[1]. Colquhoun A , et al. Differential activity of the nerve growth factor (NGF) antagonist PD90780 [7-(benzolylamino)-4,9-dihydro-4-methyl-9-oxo-pyrazolo[5,1-b]quinazoline-2-carboxylic acid] suggests altered NGF-p75NTR interactions in the presence of TrkA. J
|
| Additional Infomation |
PD 90780 is a non-peptidic NGF antagonist that disrupts NGF interaction with the p75 neurotrophin receptor. Its mechanism involves direct binding to NGF, preventing NGF from binding to p75^NTR^. The compound is a valuable research tool for studying NGF biology, p75^NTR^ signaling, and the role of NGF in pain, neurodegeneration, and other conditions. PD 90780 has not received regulatory approval for clinical use.
|
| Molecular Formula |
C19H14N4O4
|
|---|---|
| Molecular Weight |
362.33886384964
|
| Exact Mass |
362.102
|
| CAS # |
77422-99-2
|
| PubChem CID |
9885305
|
| Appearance |
Light yellow to yellow solid powder
|
| LogP |
2.209
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
27
|
| Complexity |
621
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C1C2C=C(C=CC=2N(C)C2=CC(C(=O)O)=NN21)NC(C1C=CC=CC=1)=O
|
| InChi Key |
IAZAGXDMMVWYKF-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H14N4O4/c1-22-15-8-7-12(20-17(24)11-5-3-2-4-6-11)9-13(15)18(25)23-16(22)10-14(21-23)19(26)27/h2-10H,1H3,(H,20,24)(H,26,27)
|
| Chemical Name |
7-benzamido-4-methyl-9-oxopyrazolo[5,1-b]quinazoline-2-carboxylic acid
|
| Synonyms |
PD 90780; PD-90780; PD90780
|
| 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) |
DMSO : ~31.25 mg/mL (~86.24 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 | 2.7598 mL | 13.7992 mL | 27.5984 mL | |
| 5 mM | 0.5520 mL | 2.7598 mL | 5.5197 mL | |
| 10 mM | 0.2760 mL | 1.3799 mL | 2.7598 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
COA