2014/11/21
Dorsomorphin 2HCl Datasheet
Dorsomorphin 2HCl Chemical Structure
Dorsomorphin 2HCl
Catalog No.S7306
Technical Data
Molecular Weight (MW)
472.41
Formula
C24H25N5O.2HCl
Solubility (25°C)
* <1 mg/ml means slightly
soluble or insoluble
CAS No.
1219168-18-9
Synonyms
BML-275,Compound C
DMSO <1 mg/mL (<1 mM)
Water 94 mg/mL (198.97 mM)
Ethanol <1 mg/mL (<1 mM)
3 years
-20℃ Powder
Storage
6 months -80℃ in DMSO
Return Policy
Selleck Chemical’s Unconditional
Chemical Name
Return Policy ensures a smooth online
6-[4-[2-(1-Piperidinyl)ethoxy]pheny​
l]-3-(4-pyridinyl)-pyrazolo[1,5-a]pyrimidine dihydrochloride
shopping experience for our customers.
If you are in any way unsatisfied with
Preparing Stock Solutions
your purchase, you may return any
item(s) within 365 days of its original
1 mg
5 mg
10 mg
1 mM
2.1168 mL
10.5840 mL
21.1681 mL
5 mM
0.4234 mL
2.1168 mL
4.2336 mL
10 mM
0.2117 mL
1.0584 mL
2.1168 mL
-- USA and Canada only --
50 mM
0.0423 mL
0.2117 mL
0.4234 mL
Fax:
purchase date.
Toll Free:
(877) 796-6397
+1-713-796-9816
Biological Activity
Description
Orders:
Dorsomorphin is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM, exhibiting no significant
inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits BMP
type I receptor.
[email protected]
Tech Support:
+1-832-582-8158 Ext:3
Targets
AMPK
IC50
109 nM [1]
In vitro
Dorsomorphin inhibits ACC inactivation by either AICAR or metformin, and also attenuates AICAR and
metformin’s effect to increase fatty acid oxidation or suppress lipogenic genes in hepatocytes. [1] Inhibition of
AMPK activity by Dorsomorphin almost completely inhibits autophagic proteolysis in HT-29 cells. [2] in addition,
[email protected]
(Please provide your Order Number in
Dorsomorphin selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6, and thus blocks BMP[3]
mediated SMAD1/5/8 phosphorylation, target gene transcription and osteogenic differentiation.
In vivo
+1-832-582-8158
the email. We strive to reply to all email
inquiries within one business day.)
Website:
www.selleckchem.com
Dorsomorphin (10 mg/kg) reduces basal levels of hepcidin expression and increases serum iron concentrations
[3]
in adult mice.
Dorsomorphin (0.2 mg/kg, i.v.) significantly reduces VCAM-1 and ICAM-1 expression in the
thoracic aorta of LPS-treated rats. [4]
Features
Protocol (Only for Reference)
Kinase Assay: [1]
Liver AMPK is partially purified from male SD rats to the blue-Sepharose step. The 100-μl reaction mixture
contains 100 μM AMP, 100 μM ATP (0.5 μCi 33P-ATP per reaction), and 50 μM SAMS in a buffer (40 mM HEPES,
pH 7.0, 80 mM NaCl, 0.8 mM EDTA, 5 mM MgCl2, 0.025% BSA, and 0.8 mM DTT). The reaction is initiated with
addition of the enzyme. After 30-minute incubation at 30°C, the reaction is stopped by addition of 80 μl 1%
AMPK partial
purification and in
vitro kinase assay.
H3PO4. Aliquots (100 μl) are transferred to 96-well MultiScreen plates. The plate is washed three times with 1%
H3PO4 followed by detection in a Top-count. The in vitro AMPK inhibition data obtained with compound C — (6[4-(2-Piperidin-1-yl-ethoxy)-phenyl)]-3-pyridin-4-yl-pyyrazolo[1,5-a] pyrimidine — are fit to the following equation
for competitive inhibition by nonlinear regression using a least-squares Marquardt algorithm in a computer
program written by N. Thornberry of Merck Research Laboratories: Vi/Vo = (Km + S)/[S + Km × (1 + I/Ki)], where Vi
is the inhibited velocity, Vo is the initial velocity, S is the substrate (ATP) concentration, Km is the Michaelis
constant for ATP, I is the inhibitor (compound C) concentration, and Ki is the dissociation constant for compound
C.
Animal Study: [3]
Animal Models
Iron-replete mice
Formulation
DMSO
Dosages
~10 mg/kg
Administration
i.v.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species
Baboon
Dog
Monkey
Rabbit
http://www.selleckchem.com/datasheet/dorsomorphin-2hcl-DataSheet.html
Guinea pig
Rat
Hamster
Mouse
1/2
2014/11/21
Dorsomorphin 2HCl Datasheet
Weight (kg)
12
10
3
1.8
0.4
0.15
0.08
0.02
2
Body Surface Area (m )
0.6
0.5
0.24
0.15
0.05
0.025
0.02
0.007
Km factor
20
20
12
12
8
6
5
3
Animal A (mg/kg) = Animal B (mg/kg) multiplied by
Animal B Km
Animal A Km
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by
the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2
mg/kg.
Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×
mouse Km(3)
rat Km(6)
= 11.2 mg/kg
References
[1] Zhou G, et al. J Clin Invest. 2001, 108(8), 1167-1174.
[2] Meley D, et al. J Biol Chem. 2006, 281(46), 34870-34879.
[3] Yu PB, et al. Nat Chem Biol. 2008, 4(1), 33-41.
[4] Kim YM, et al. Atherosclerosis. 2011, 219(1), 57-64.
PLEASE KEEP THE PRODUCT UNDER -20°C FOR LONG-TERM STORAGE.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE
Specific storage and handling information for each product is indicated on the product datasheet. Most Selleck products are stable under
the recommended conditions. Products are sometimes shipped at a temperature that differs from the recommended storage temperature.
Short-term storage of many products are stable in the short-term at temperatures that differ from that required for long-term storage.
We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt of the product, follow the
storage recommendations on the product data sheet.
http://www.selleckchem.com/datasheet/dorsomorphin-2hcl-DataSheet.html
2/2