3-PYRIDINECARBOXAMIDE, 6-(3-FLUOROPHENYL)-N-[1-(2,2,2-TRIFLUOROETHYL)-4-PIPERIDINYL]-
- Product Name
- 3-PYRIDINECARBOXAMIDE, 6-(3-FLUOROPHENYL)-N-[1-(2,2,2-TRIFLUOROETHYL)-4-PIPERIDINYL]-
- CAS No.
- 1033836-12-2
- Chemical Name
- 3-PYRIDINECARBOXAMIDE, 6-(3-FLUOROPHENYL)-N-[1-(2,2,2-TRIFLUOROETHYL)-4-PIPERIDINYL]-
- Synonyms
- CS-1438;MDK36122;HPGDS inhibitor 1;HPGDS inhibitor 1, >=98%;Prostaglandin D Synthase (hematopoietic-type) Inhibitor I;6-(3-fluorophenyl)-N-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)nicotinaMide;6-(3-Fluorophenyl)-N-[1-(2,2,2-trifluoroethyl)-4-piperidinyl]-3-pyridinecarboxamide;3-PYRIDINECARBOXAMIDE, 6-(3-FLUOROPHENYL)-N-[1-(2,2,2-TRIFLUOROETHYL)-4-PIPERIDINYL]-
- CBNumber
- CB22599009
- Molecular Formula
- C19H19F4N3O
- Formula Weight
- 381.37
- MOL File
- 1033836-12-2.mol
3-PYRIDINECARBOXAMIDE, 6-(3-FLUOROPHENYL)-N-[1-(2,2,2-TRIFLUOROETHYL)-4-PIPERIDINYL]- Property
- Boiling point:
- 487.2±45.0 °C(Predicted)
- Density
- 1.33±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- Soluble in DMSO
- form
- crystalline solid
- pka
- 9.55±0.20(Predicted)
- color
- White to off-white
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing 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.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
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.
P321Specific treatment (see … on this label).
P330Rinse mouth.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 16256
- Product name
- Prostaglandin D Synthase (hematopoietic-type) Inhibitor I
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $121
- Updated
- 2024/03/01
- Product number
- 16256
- Product name
- Prostaglandin D Synthase (hematopoietic-type) Inhibitor I
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $302
- Updated
- 2024/03/01
- Product number
- 16256
- Product name
- Prostaglandin D Synthase (hematopoietic-type) Inhibitor I
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $543
- Updated
- 2024/03/01
- Product number
- orb181253
- Product name
- HPGDS-inhibitor-1
- Purity
- >98%
- Packaging
- 100mg
- Price
- $765
- Updated
- 2021/12/16
- Product number
- orb181253
- Product name
- HPGDS-inhibitor-1
- Purity
- >98%
- Packaging
- 250mg
- Price
- $1504.5
- Updated
- 2021/12/16
3-PYRIDINECARBOXAMIDE, 6-(3-FLUOROPHENYL)-N-[1-(2,2,2-TRIFLUOROETHYL)-4-PIPERIDINYL]- Chemical Properties,Usage,Production
Biological Activity
hpgds inhibitor 1 is an oral potent and selective inhibitor of hematopoietic prostaglandin d synthase (hpgds) with ic50 value of 0.7nm [1].prostaglandin d2 (pgd2) is a mediator of allergy and inflammation. it is isomerized from pgh2 by pgds. this production is important in airway allergic and inflammatory processes. hpgds inhibitor 1 has a 3-fluorine substituent, making it stable in the in vitro human microsome assay. it has potent effects in enzyme assay and cellular assay with ic50 values of 0.7nm and 32nm, respectively. in addition, the potency is equal against purified hpgds from various species with ic50 values ranging from 0.5-2.3nm. besides that, hpgds inhibitor 1 is selective against hpgds over other relevant human enzymes including l-pgds, mpges, cox-1, cox-2 and 5 lox [1].in a model of antigen-induced airway response in allergic sheep, treatment of hpgds inhibitor 1 completely prevents the late asthma reaction and blocks the airway hyper-responsiveness [1].
in vitro
HPGDS inhibitor 1 has equal potency against purified HPGDS from human, rat, dog, and sheep (IC 50 , 0.5-2.3 nM).
in vivo
HPGDS inhibitor 1 (compound 8; 1 mg/kg) has excellent PK characteristics with 76% bioavailability, and the T 1/2 is 4.1 hours in rats.
Rats dosed orally with 1 mg/kg and 10 mg/kg HPGDS inhibitor 1 (compound 8) are sacrificed at various times. Oral administration of it blocks PGD2 production in the rat spleen; inhibition of PGD2 is inversely correlated with the plasma concentration of it in a time- and dose-dependent manner.
It (compound 8; 1 mg/mL) illustrates efficacy in an in vivo sheep model of asthma.
target
IC50: 0.6 nM (HPGDS in enzyme assays) and 32 nM (HPGDS in cellular assays)
References
[1] carron c p, trujillo j i, olson k l, et al. discovery of an oral potent selective inhibitor of hematopoietic prostaglandin d synthase (hpgds). acs medicinal chemistry letters, 2010, 1(2): 59-63.
3-PYRIDINECARBOXAMIDE, 6-(3-FLUOROPHENYL)-N-[1-(2,2,2-TRIFLUOROETHYL)-4-PIPERIDINYL]- Preparation Products And Raw materials
Raw materials
Preparation Products
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- Product
- 3-PYRIDINECARBOXAMIDE, 6-(3-FLUOROPHENYL)-N-[1-(2,2,2-TRIFLUOROETHYL)-4-PIPERIDINYL]- 1033836-12-2
- Price
- US $9.80/KG
- Min. Order
- 1g
- Purity
- ≥99%
- Supply Ability
- 100kg
- Release date
- 2019-12-24