| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
PD173212 targets N-type voltage-sensitive calcium channels (VSCC, Cav2.2). The compound is a selective N-type calcium channel blocker with an IC₅₀ of 36 nM in IMR-32 assays. By blocking N-type calcium channels, PD173212 inhibits calcium influx into neurons, reducing neurotransmitter release and modulating pain signaling.
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| ln Vitro |
PD173212 (PD 173212, 300 nM) has an IC50 of 74 nM and can efficiently block recombinant class B (N-type) calcium channel currents by 78±7.8% when using whole-cell voltage clamp technology. Comparing neuronal Na+, K+, and L-type Ca2+ channels to non-L-type Ca2+ channels, PD 173212 is selective for these channels [1].
In vitro, PD173212 demonstrates potent and selective blockade of N-type calcium channels with an IC₅₀ of 36 nM in IMR-32 assays. The compound's selectivity for N-type over other calcium channel subtypes contributes to its pharmacological profile. By inhibiting calcium influx through Cav2.2 channels, PD173212 reduces neurotransmitter release from primary afferent neurons. |
| ln Vivo |
In an audiogenic seizure model, PD173212 (30 mg/kg, intravenously) demonstrated a moderate level of efficacy in preventing tonic seizures [1].
In vivo, PD173212 (0.0017-1.7 µmol/kg, intraperitoneal) significantly reduces visceral hypersensitivity in a DNBS-induced colitis mouse model. The compound also prevents audiogenic seizures in mice when administered at a dose of 30 mg/kg. These findings support the role of N-type calcium channels in pain and seizure modulation. |
| Enzyme Assay |
In vitro electrophysiological assays for N-type calcium channel blockade involve patch-clamp recording of Cav2.2 channels expressed in heterologous systems (e.g., HEK-293 cells) or in IMR-32 neuroblastoma cells. PD173212 is applied at varying concentrations, and the inhibition of calcium currents is measured. IC₅₀ values are calculated from dose-response curves.
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| Cell Assay |
Cellular assays are performed using IMR-32 cells or other neuronal cell lines expressing N-type calcium channels. Cells are treated with PD173212 at various concentrations, and calcium influx is measured using calcium-sensitive fluorescent dyes upon depolarization. The compound's ability to inhibit calcium influx through N-type channels is determined.
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| Animal Protocol |
In vivo studies are conducted in rodent models of pain and seizures. In the DNBS-induced colitis model, PD173212 is administered intraperitoneally at 0.0017-1.7 µmol/kg, and visceral hypersensitivity is assessed. In the audiogenic seizure model, the compound is administered at 30 mg/kg, and seizure prevention is evaluated.
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| ADME/Pharmacokinetics |
PD173212 (molecular weight 599.85, formula C₃₈H₅₃N₃O₃) is a small-molecule compound. It is soluble in DMSO and is typically stored at -20°C. Its physicochemical properties support its use in both in vitro and in vivo studies.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of PD173212 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 N-type calcium channel function.
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| References | |
| Additional Infomation |
PD173212 is a selective N-type voltage-sensitive calcium channel blocker. Its mechanism involves blocking Cav2.2 channels, reducing calcium influx and neurotransmitter release. The compound has demonstrated efficacy in reducing visceral hypersensitivity and preventing audiogenic seizures in preclinical models. PD173212 is primarily used for research purposes and has not received regulatory approval for clinical use.
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| Molecular Formula |
C38H53N3O3
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|---|---|
| Molecular Weight |
599.84572
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| Exact Mass |
599.409
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| Elemental Analysis |
C, 76.09; H, 8.91; N, 7.01; O, 8.00
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| CAS # |
217171-01-2
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| PubChem CID |
9916734
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| Appearance |
White to off-white solid powder
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| LogP |
7.833
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
44
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| Complexity |
854
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O=C(NC(C)(C)C)[C@@H](NC([C@H](CC(C)C)N(C)CC1=CC=C(C(C)(C)C)C=C1)=O)CC2=CC=C(OCC3=CC=CC=C3)C=C2
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| InChi Key |
WJAVQCPRFGVNSN-HEVIKAOCSA-N
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| InChi Code |
InChI=1S/C38H53N3O3/c1-27(2)23-34(40(9)25-29-15-19-31(20-16-29)37(3,4)5)36(43)41(38(6,7)8)33(35(39)42)24-28-17-21-32(22-18-28)44-26-30-13-11-10-12-14-30/h10-22,27,33-34H,23-26H2,1-9H3,(H2,39,42)/t33-,34-/m0/s1
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| Chemical Name |
(S)-N-((S)-1-amino-3-(4-(benzyloxy)phenyl)-1-oxopropan-2-yl)-N-(tert-butyl)-2-((4-(tert-butyl)benzyl)(methyl)amino)-4-methylpentanamide
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| Synonyms |
PD-173212; PD 173212; PD173212;
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| HS Tariff Code |
2934.99.03.00
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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 : ≥ 100 mg/mL (~166.71 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6671 mL | 8.3354 mL | 16.6708 mL | |
| 5 mM | 0.3334 mL | 1.6671 mL | 3.3342 mL | |
| 10 mM | 0.1667 mL | 0.8335 mL | 1.6671 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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