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MedKoo Cat#: 527777 | Name: PH-002
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

PH-002 is a novel inhibitor of apolipoprotein (apo) E4 intramolecular domain interaction in neuronal cells that restores mitochondrial cytochrome c oxidase subunit 1 levels, rescuing impairments of mitochondrial motility and neurite outgrowth. Administration of PH-002 significantly improved motor function in old mice.

Chemical Structure

PH-002
PH-002
CAS#1311174-68-1

Theoretical Analysis

MedKoo Cat#: 527777

Name: PH-002

CAS#: 1311174-68-1

Chemical Formula: C27H33N5O4

Exact Mass: 491.2533

Molecular Weight: 491.59

Elemental Analysis: C, 65.97; H, 6.77; N, 14.25; O, 13.02

Price and Availability

Size Price Availability Quantity
50mg USD 550.00 2 Weeks
100mg USD 950.00 2 Weeks
200mg USD 1,450.00 2 Weeks
500mg USD 2,150.00 2 Weeks
1g USD 3,350.00 2 Weeks
2g USD 5,950.00 2 Weeks
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Related CAS #
No Data
Synonym
PH-002; PH 002; PH002
IUPAC/Chemical Name
4-[[4-[[2-(3,4-Dihydro-3-methyl-4-oxo-1-phthalazinyl)acetyl]amino]phenyl]methyl]-1-piperazinecarboxylic acid 1,1-dimethylethyl ester
InChi Key
GSXXTLWPQMHHDJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C27H33N5O4/c1-27(2,3)36-26(35)32-15-13-31(14-16-32)18-19-9-11-20(12-10-19)28-24(33)17-23-21-7-5-6-8-22(21)25(34)30(4)29-23/h5-12H,13-18H2,1-4H3,(H,28,33)
SMILES Code
O=C(N1CCN(CC2=CC=C(NC(CC3=NN(C)C(C4=C3C=CC=C4)=O)=O)C=C2)CC1)OC(C)(C)C
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
PH-002 is an inhibitor of apolipoprotein (apo) E4 intramolecular domain interaction.
In vitro activity:
The intracellular trafficking of apoE4 is impaired in Neuro-2a cells and primary neurons, as shown by measuring fluorescence recovery after photobleaching. The trafficking impairment of apoE4 was also rescued by disrupting domain interaction with the small-molecule structure correctors GIND25 and PH002. PH002 also rescued apoE4-induced impairments of neurite outgrowth in Neuro-2a cells and dendritic spine development in primary neurons. Reference: J Biol Chem. 2011 May 13;286(19):17217-26. https://pubmed.ncbi.nlm.nih.gov/21454574/
In vivo activity:
TBD
Solvent mg/mL mM comments
Solubility
DMF 15.0 30.51
DMF:PBS (pH 7.2) (1:9) 0.1 0.20
DMSO 61.0 124.09
Ethanol 17.5 35.60
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 491.59 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Chen HK, Liu Z, Meyer-Franke A, Brodbeck J, Miranda RD, McGuire JG, Pleiss MA, Ji ZS, Balestra ME, Walker DW, Xu Q, Jeong DE, Budamagunta MS, Voss JC, Freedman SB, Weisgraber KH, Huang Y, Mahley RW. Small molecule structure correctors abolish detrimental effects of apolipoprotein E4 in cultured neurons. J Biol Chem. 2012 Feb 17;287(8):5253-66. doi: 10.1074/jbc.M111.276162. Epub 2011 Dec 12. PMID: 22158868; PMCID: PMC3285306. 2. Brodbeck J, McGuire J, Liu Z, Meyer-Franke A, Balestra ME, Jeong DE, Pleiss M, McComas C, Hess F, Witter D, Peterson S, Childers M, Goulet M, Liverton N, Hargreaves R, Freedman S, Weisgraber KH, Mahley RW, Huang Y. Structure-dependent impairment of intracellular apolipoprotein E4 trafficking and its detrimental effects are rescued by small-molecule structure correctors. J Biol Chem. 2011 May 13;286(19):17217-26. doi: 10.1074/jbc.M110.217380. Epub 2011 Mar 18. PMID: 21454574; PMCID: PMC3089564.
In vitro protocol:
1. Chen HK, Liu Z, Meyer-Franke A, Brodbeck J, Miranda RD, McGuire JG, Pleiss MA, Ji ZS, Balestra ME, Walker DW, Xu Q, Jeong DE, Budamagunta MS, Voss JC, Freedman SB, Weisgraber KH, Huang Y, Mahley RW. Small molecule structure correctors abolish detrimental effects of apolipoprotein E4 in cultured neurons. J Biol Chem. 2012 Feb 17;287(8):5253-66. doi: 10.1074/jbc.M111.276162. Epub 2011 Dec 12. PMID: 22158868; PMCID: PMC3285306. 2. Brodbeck J, McGuire J, Liu Z, Meyer-Franke A, Balestra ME, Jeong DE, Pleiss M, McComas C, Hess F, Witter D, Peterson S, Childers M, Goulet M, Liverton N, Hargreaves R, Freedman S, Weisgraber KH, Mahley RW, Huang Y. Structure-dependent impairment of intracellular apolipoprotein E4 trafficking and its detrimental effects are rescued by small-molecule structure correctors. J Biol Chem. 2011 May 13;286(19):17217-26. doi: 10.1074/jbc.M110.217380. Epub 2011 Mar 18. PMID: 21454574; PMCID: PMC3089564.
In vivo protocol:
TBD
1: Yorke J, Deaton C, Campbell M, McGowen L, Sephton P, Kiely DG, Armstrong I. Symptom severity and its effect on health-related quality of life over time in patients with pulmonary hypertension: a multisite longitudinal cohort study. BMJ Open Respir Res. 2018 Mar 1;5(1):e000263. doi: 10.1136/bmjresp-2017-000263. eCollection 2018. PubMed PMID: 29531745; PubMed Central PMCID: PMC5844371. 2: Abouelnour AE, Doyle M, Thompson DV, Yamrozik J, Williams RB, Shah MB, Soma SK, Murali S, Benza RL, Biederman RW. Does Late Gadolinium Enhancement still have Value? Right Ventricular Internal Mechanical Work, E(a)/E(max) and Late Gadolinium Enhancement as Prognostic Markers in Patients with Advanced Pulmonary Hypertension via Cardiac MRI. Cardiol Res Cardiovasc Med. 2017;2017(1). pii: CRCM-111. Epub 2017 Jan 11. PubMed PMID: 29528042. 3: Das S, Chatterjee P, Ghangrekar MM. Increasing methane content in biogas and simultaneous value added product recovery using microbial electrosynthesis. Water Sci Technol. 2018 Mar;77(5):1293-1302. doi: 10.2166/wst.2018.002. PubMed PMID: 29528317; PubMed Central PMCID: wst_2018_002. 4: Er A, Çağlar A, Akgül F, Ulusoy E, Çitlenbik H, Yılmaz D, Duman M. Early predictors of unresponsiveness to high-flow nasal cannula therapy in a pediatric emergency department. Pediatr Pulmonol. 2018 Mar 12. doi: 10.1002/ppul.23981. [Epub ahead of print] PubMed PMID: 29528202. 5: Asferg CL, Nielsen SJ, Andersen UB, Linneberg A, Goetze JP, Jeppesen JL. Serum proatrial natriuretic peptide concentrations during oral glucose-induced acute hyperinsulinemia in lean and obese men. Peptides. 2018 Mar 7. pii: S0196-9781(18)30044-5. doi: 10.1016/j.peptides.2018.03.005. [Epub ahead of print] PubMed PMID: 29524563. 6: Chouinard VA, Henderson DC, Dalla Man C, Valeri L, Gray BE, Ryan KP, Cypess AM, Cobelli C, Cohen BM, Öngür D. Impaired insulin signaling in unaffected siblings and patients with first-episode psychosis. Mol Psychiatry. 2018 Mar 9. doi: 10.1038/s41380-018-0045-1. [Epub ahead of print] PubMed PMID: 29523870. 7: Xu X, Zhang G, Hu M, Ji C, Meng J, Lai Z, Dai M, Pang L, Zhang W. [Influence of clinical nutritional support on the effects of mechanical ventilation]. Zhonghua Wei Zhong Bing Ji Jiu Yi Xue. 2018 Mar;30(3):262-265. doi: 10.3760/cma.j.issn.2095-4352.2018.03.014. Chinese. PubMed PMID: 29519287. 8: Allou N, Lo Pinto H, Persichini R, Bouchet B, Braunberger E, Lugagne N, Belmonte O, Martinet O, Delmas B, Dangers L, Allyn J. Cannula-Related Infection in Patients Supported by Peripheral ECMO: Clinical and Microbiological Characteristics. ASAIO J. 2018 Mar 5. doi: 10.1097/MAT.0000000000000771. [Epub ahead of print] PubMed PMID: 29517513. 9: Danielsen KV, Wiese S, Hove J, Bendtsen F, Møller S. Pronounced Coronary Arteriosclerosis in Cirrhosis: Influence on Cardiac Function and Survival? Dig Dis Sci. 2018 Mar 8. doi: 10.1007/s10620-018-5006-7. [Epub ahead of print] PubMed PMID: 29516327. 10: Goni L, Sun D, Heianza Y, Wang T, Huang T, Martínez JA, Shang X, Bray GA, Smith SR, Sacks FM, Qi L. A circadian rhythm-related MTNR1B genetic variant modulates the effect of weight-loss diets on changes in adiposity and body composition: the POUNDS Lost trial. Eur J Nutr. 2018 Mar 7. doi: 10.1007/s00394-018-1660-y. [Epub ahead of print] PubMed PMID: 29516223. 11: Zurek AD, Alfaro MF, Wee AG, Yuan JC, Barao VA, Mathew MT, Sukotjo C. Wear Characteristics and Volume Loss of CAD/CAM Ceramic Materials. J Prosthodont. 2018 Mar 6. doi: 10.1111/jopr.12782. [Epub ahead of print] PubMed PMID: 29508487. 12: Sheean RK, McKay FC, Cretney E, Bye CR, Perera ND, Tomas D, Weston RA, Scheller KJ, Djouma E, Menon P, Schibeci SD, Marmash N, Yerbury JJ, Nutt SL, Booth DR, Stewart GJ, Kiernan MC, Vucic S, Turner BJ. Association of Regulatory T-Cell Expansion With Progression of Amyotrophic Lateral Sclerosis: A Study of Humans and a Transgenic Mouse Model. JAMA Neurol. 2018 Mar 5. doi: 10.1001/jamaneurol.2018.0035. [Epub ahead of print] PubMed PMID: 29507931. 13: Shahait M, Nassif S, Tamim H, Mukherji D, Hijazi M, El Sabban M, Khauli R, Bulbul M, Abou Kheir W, El Hajj A. Ki-67 expression predicts biochemical recurrence after radical prostatectomy in the setting of positive surgical margins. BMC Urol. 2018 Mar 5;18(1):13. doi: 10.1186/s12894-018-0330-y. PubMed PMID: 29506507; PubMed Central PMCID: PMC5838874. 14: Yue H, Xu Q, Xie S. High EMP3 expression might independently predict poor overall survival in glioblastoma and its expression is related to DNA methylation. Medicine (Baltimore). 2018 Jan;97(1):e9538. doi: 10.1097/MD.0000000000009538. PubMed PMID: 29505529. 15: Kang X, Zeng Y, Liang J, Li J, Ren D, Chai L, Sun Z, Yu S, Wu X, Han W, Wang W. Aberrations and clinical significance of BRAF in malignant melanoma: A series of 60 cases in Chinese Uyghur. Medicine (Baltimore). 2018 Jan;97(1):e9509. doi: 10.1097/MD.0000000000009509. PubMed PMID: 29505523. 16: Rahimi M, Lookzadeh S, Sadeghi R, Soltaninejad K, Shadnia S, Pajoumand A, Hassanian-Moghaddam H, Zamani N, Latifi-Pour M. Predictive Factors of Mortality in Acute Amphetamine Type Stimulants Poisoning; a Review of 226 Cases. Emerg (Tehran). 2018;6(1):e1. Epub 2018 Jan 10. PubMed PMID: 29503826; PubMed Central PMCID: PMC5827041. 17: Nafisi-Far N, Ghafouri-Fard S, Panah AST, Sayad A, Taheri M. A gender dimorphism in up-regulation of BACE1 gene expression in schizophrenia. Metab Brain Dis. 2018 Mar 3. doi: 10.1007/s11011-018-0205-7. [Epub ahead of print] PubMed PMID: 29500546. 18: Shaban M, Mohamed F, Abdallah S. Production and Characterization of Superhydrophobic and Antibacterial Coated Fabrics Utilizing ZnO Nanocatalyst. Sci Rep. 2018 Mar 2;8(1):3925. doi: 10.1038/s41598-018-22324-7. PubMed PMID: 29500470; PubMed Central PMCID: PMC5834644. 19: Castro P, Azevedo E, Rocha I, Sorond F, Serrador JM. Chronic kidney disease and poor outcomes in ischemic stroke: is impaired cerebral autoregulation the missing link? BMC Neurol. 2018 Mar 2;18(1):21. doi: 10.1186/s12883-018-1025-4. PubMed PMID: 29499637; PubMed Central PMCID: PMC5834853. 20: Kordestani Z, Sanjari M, Safavi M, Mashrouteh M, Asadikaram G, FekriSoofiAbadi M, Mirzazadeh A. ENHANCED BETA-CATENIN EXPRESSION IS ASSOCIATED WITH THE RECURRENCE OF PAPILLARY THYROID CARCINOMA. Endocr Pract. 2018 Mar 2. doi: 10.4158/EP171983.OR. [Epub ahead of print] PubMed PMID: 29498921.