PD 145305 Property

Melting point:

46 °C

Boiling point:

184-187 °C(Press: 11-12 Torr)

Density 

1.232±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide

pka

3.60±0.10(Predicted)

form 

solution in ethanol.

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H302Harmful if swallowed

H314Causes severe skin burns and eye damage

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P301+P330+P331IF SWALLOWED: Rinse mouth. Do NOT induce vomiting.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P303+P361+P353IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P310Immediately call a POISON CENTER or doctor/physician.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P363Wash contaminated clothing before reuse.

P405Store locked up.

P501Dispose of contents/container to..…

PD 145305 Chemical Properties,Usage,Production

Uses

PD 145305 is an inactive analog of PD 150606 , a selective inhibitor of calpains (Kis = 0.21 and 0.37 μM for μ- and m-calpain, respectively). It is inactive at concentrations up to 500 μM.

Biological Activity

pd 145305 is an inactive analog of pd 150606, a potent and selective calpains inhibitor [1].calpain is a class of cytosolic cysteine protease that is activated by elevated intracellular calcium. overactivation of calpain has been implicated in the pathophysiology of several degenerative conditions, including stroke, myocardial ischemia, neuromuscular degeneration, and cataract formation [1].pd 145305 is an inactive analog of pd 150606, a potent and selective calpains inhibitor. pd 150606, an alpha-mercaptoacrylate derivative, inhibited μ-calpain and m-calpain with ki values of 0.21 and 0.37 μm, respectively. pd 145305 was inactive at concentrations up to 500 μm. in human leukemic molt-4 cells, pd150606 inhibited a-spectrin proteolysis in a dose-dependent way and virtually eliminated the formation of the 145-kda fragment at 10 μm, whereas pd145305 did not attenuate a-spectrin breakdown product formation. in fetal rat cerebrocortical cultures subjected to a combination of hypoxia and hypoglycemia, pd150606 significantly inhibited the release of lactate dehydrogenase, whereas pd145305 was ineffective. pd150606, but not pd145305, was found to make cerebral glutamatergic neurons more resistant to hypoxic/hypoglycemic challenge [1].

References

[1]. wang kk, nath r, posner a, et al. an alpha-mercaptoacrylic acid derivative is a selective nonpeptide cell-permeable calpain inhibitor and is neuroprotective. proc natl acad sci u s a. 1996 jun 25;93(13):6687-92.